PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 19755386-5 2009 EXPERIMENTAL DESIGN: We tested the expression of Src tyrosine kinase in Waldenstrom macroglobulinemia and normal cells, and the effect of the specific Src inhibitor AZD0530 on the adhesion, migration, cell cycle, and survival of a Waldenstrom macroglobulinemia cell line and patient samples. saracatinib 165-172 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 151-154 19755386-7 2009 RESULTS: We show that Src is overexpressed in Waldenstrom macroglobulinemia cells compared with control B cells, and that the use of the Src inhibitor AZD0530 led to significant inhibition of adhesion, migration, and cytoskeletal signaling induced by SDF1. saracatinib 151-158 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 22-25 19755386-7 2009 RESULTS: We show that Src is overexpressed in Waldenstrom macroglobulinemia cells compared with control B cells, and that the use of the Src inhibitor AZD0530 led to significant inhibition of adhesion, migration, and cytoskeletal signaling induced by SDF1. saracatinib 151-158 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 137-140 19755386-7 2009 RESULTS: We show that Src is overexpressed in Waldenstrom macroglobulinemia cells compared with control B cells, and that the use of the Src inhibitor AZD0530 led to significant inhibition of adhesion, migration, and cytoskeletal signaling induced by SDF1. saracatinib 151-158 C-X-C motif chemokine ligand 12 Homo sapiens 251-255 34883449-8 2022 Accordingly, the inhibition of the SRC signaling pathway by saracatinib blocked periplocin-induced proliferation and lipid accumulation in meibomian gland cells. saracatinib 60-71 Rous sarcoma oncogene Mus musculus 35-38 34798298-1 2022 OBJECTIVE: To observe the effect of AZD0530 on the progression of knee OA after blocking beta-catenin phosphorylation and then dormancy of the Wnt/beta pathway by tyrosine kinase Fyn. saracatinib 36-43 catenin beta 1 Homo sapiens 89-101 34798298-1 2022 OBJECTIVE: To observe the effect of AZD0530 on the progression of knee OA after blocking beta-catenin phosphorylation and then dormancy of the Wnt/beta pathway by tyrosine kinase Fyn. saracatinib 36-43 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 179-182 34798298-6 2022 The levels of beta-catenin, p-beta-catenin (Tyr142) and MMP13 in chondrocytes decreased, while the level of Aggrecan increased after AZD0530 was used to intervene chondrocytes in vitro, which was positively correlated with the dose of AZD0530. saracatinib 133-140 catenin beta 1 Homo sapiens 14-26 34798298-6 2022 The levels of beta-catenin, p-beta-catenin (Tyr142) and MMP13 in chondrocytes decreased, while the level of Aggrecan increased after AZD0530 was used to intervene chondrocytes in vitro, which was positively correlated with the dose of AZD0530. saracatinib 133-140 catenin beta 1 Homo sapiens 30-42 34798298-6 2022 The levels of beta-catenin, p-beta-catenin (Tyr142) and MMP13 in chondrocytes decreased, while the level of Aggrecan increased after AZD0530 was used to intervene chondrocytes in vitro, which was positively correlated with the dose of AZD0530. saracatinib 133-140 matrix metallopeptidase 13 Homo sapiens 56-61 34798298-9 2022 AZD0530 can inhibit tyrosine kinase Fyn from beta-catenin phosphorylation, a key Wnt/beta pathway protein, and then inhibit Wnt/beta pathway levels in chondrocytes. saracatinib 0-7 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 36-39 34798298-9 2022 AZD0530 can inhibit tyrosine kinase Fyn from beta-catenin phosphorylation, a key Wnt/beta pathway protein, and then inhibit Wnt/beta pathway levels in chondrocytes. saracatinib 0-7 catenin beta 1 Homo sapiens 45-57 34830154-8 2021 In mouse TG, a SFKs inhibitor, saracatinib, restored the CGRP release and IL-1beta mRNA level increased by a TRPA1 activator, umbellulone. saracatinib 31-42 calcitonin/calcitonin-related polypeptide, alpha Mus musculus 57-61 34830154-8 2021 In mouse TG, a SFKs inhibitor, saracatinib, restored the CGRP release and IL-1beta mRNA level increased by a TRPA1 activator, umbellulone. saracatinib 31-42 interleukin 1 alpha Mus musculus 74-82 34830154-8 2021 In mouse TG, a SFKs inhibitor, saracatinib, restored the CGRP release and IL-1beta mRNA level increased by a TRPA1 activator, umbellulone. saracatinib 31-42 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 109-114 34158343-1 2021 AZD0530, a potent small-molecule inhibitor of Src family kinases, is an anti-cancer drug used in the treatment of various cancers. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 46-49 34475522-0 2022 Effects of the Fyn kinase inhibitor saracatinib on ventral striatal activity during performance of an fMRI monetary incentive delay task in individuals family history positive or negative for alcohol use disorder. saracatinib 36-47 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 15-18 34158343-4 2021 We show that Src activity of GBM and GSC is increased by radiation and inhibited by AZD0530, and using clonogenic assays, AZD0530 enhances the radiosensitivity of GBM and GSCs. saracatinib 84-91 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 13-16 34158343-4 2021 We show that Src activity of GBM and GSC is increased by radiation and inhibited by AZD0530, and using clonogenic assays, AZD0530 enhances the radiosensitivity of GBM and GSCs. saracatinib 122-129 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 13-16 34158343-6 2021 Additionally, AZD0530 was shown to inhibit the radiation-induced EGFR/PI3K/AKT pathway which in known to promote and regulate radioresistance and survival of GBM cells by radiation. saracatinib 14-21 epidermal growth factor receptor Homo sapiens 65-69 34158343-6 2021 Additionally, AZD0530 was shown to inhibit the radiation-induced EGFR/PI3K/AKT pathway which in known to promote and regulate radioresistance and survival of GBM cells by radiation. saracatinib 14-21 AKT serine/threonine kinase 1 Homo sapiens 75-78 34531767-4 2021 The Src/Fyn kinase inhibitor saracatinib (AZD0530) reduces ethanol self-administration and enhances extinction of goal-directed ethanol-seeking in mice. saracatinib 29-40 Fyn proto-oncogene Mus musculus 8-11 34531767-4 2021 The Src/Fyn kinase inhibitor saracatinib (AZD0530) reduces ethanol self-administration and enhances extinction of goal-directed ethanol-seeking in mice. saracatinib 42-49 Fyn proto-oncogene Mus musculus 8-11 34087381-0 2021 Mechanisms of disease-modifying effect of saracatinib (AZD0530), a Src/Fyn tyrosine kinase inhibitor, in the rat kainate model of temporal lobe epilepsy. saracatinib 42-53 FYN proto-oncogene, Src family tyrosine kinase Rattus norvegicus 71-74 34087381-0 2021 Mechanisms of disease-modifying effect of saracatinib (AZD0530), a Src/Fyn tyrosine kinase inhibitor, in the rat kainate model of temporal lobe epilepsy. saracatinib 55-62 FYN proto-oncogene, Src family tyrosine kinase Rattus norvegicus 71-74 34087381-2 2021 In this study, we show a significant disease-modifying effect and the mechanisms of a Fyn/Src tyrosine kinase inhibitor, saracatinib (SAR, also known as AZD0530), in the rat kainate (KA) model of TLE. saracatinib 121-132 FYN proto-oncogene, Src family tyrosine kinase Rattus norvegicus 86-89 34087381-2 2021 In this study, we show a significant disease-modifying effect and the mechanisms of a Fyn/Src tyrosine kinase inhibitor, saracatinib (SAR, also known as AZD0530), in the rat kainate (KA) model of TLE. saracatinib 153-160 FYN proto-oncogene, Src family tyrosine kinase Rattus norvegicus 86-89 33705358-2 2021 From a screen of known biologically active compounds, we identified saracatinib as a potent ALK2 kinase inhibitor. saracatinib 68-79 activin A receptor, type 1 Mus musculus 92-96 33910400-3 2021 Herein, we further investigated the underlying signaling mechanism of these pro-angiogenic factors after ischemic stroke using a selective Src family inhibitor AZD0530. saracatinib 160-167 Rous sarcoma oncogene Mus musculus 139-142 33910400-6 2021 Compared to WT, AZD0530 administration exacerbated spatial cognitive impairments and brain atrophy in EC-miR-15a/16-1 cKO mice following MCAO. saracatinib 16-23 microRNA 15a Mus musculus 105-112 33910400-8 2021 Moreover, AZD0530 blocked the Src signaling pathway by downregulating phospho-Src and its downstream mediators (p-Stat3, p-Akt, p-FAK, p-p44/42 MAPK, p-p38 MAPK) in post-ischemic brains. saracatinib 10-17 Rous sarcoma oncogene Mus musculus 30-33 33910400-8 2021 Moreover, AZD0530 blocked the Src signaling pathway by downregulating phospho-Src and its downstream mediators (p-Stat3, p-Akt, p-FAK, p-p44/42 MAPK, p-p38 MAPK) in post-ischemic brains. saracatinib 10-17 Rous sarcoma oncogene Mus musculus 78-81 33910400-8 2021 Moreover, AZD0530 blocked the Src signaling pathway by downregulating phospho-Src and its downstream mediators (p-Stat3, p-Akt, p-FAK, p-p44/42 MAPK, p-p38 MAPK) in post-ischemic brains. saracatinib 10-17 signal transducer and activator of transcription 3 Mus musculus 114-119 33910400-8 2021 Moreover, AZD0530 blocked the Src signaling pathway by downregulating phospho-Src and its downstream mediators (p-Stat3, p-Akt, p-FAK, p-p44/42 MAPK, p-p38 MAPK) in post-ischemic brains. saracatinib 10-17 thymoma viral proto-oncogene 1 Mus musculus 123-126 33910400-8 2021 Moreover, AZD0530 blocked the Src signaling pathway by downregulating phospho-Src and its downstream mediators (p-Stat3, p-Akt, p-FAK, p-p44/42 MAPK, p-p38 MAPK) in post-ischemic brains. saracatinib 10-17 PTK2 protein tyrosine kinase 2 Mus musculus 130-133 33910400-8 2021 Moreover, AZD0530 blocked the Src signaling pathway by downregulating phospho-Src and its downstream mediators (p-Stat3, p-Akt, p-FAK, p-p44/42 MAPK, p-p38 MAPK) in post-ischemic brains. saracatinib 10-17 mitogen-activated protein kinase 14 Mus musculus 152-160 34589604-10 2021 Oral administration of saracatinib, a FYN kinase inhibitor, significantly suppressed formation of bone osteolytic lesions in a polyethylene debris-induced osteolysis model. saracatinib 23-34 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 38-41 33410098-0 2021 ActivinA Induced SMAD1/5 Signaling in an iPSC Derived EC Model of Fibrodysplasia Ossificans Progressiva (FOP) Can Be Rescued by the Drug Candidate Saracatinib. saracatinib 147-158 SMAD family member 1 Homo sapiens 17-24 33705358-3 2021 In enzymatic and cell-based assays, saracatinib preferentially inhibited ALK2 compared with other receptors of the BMP/TGFb signaling pathway, and induced dorsalization in zebrafish embryos consistent with BMP antagonism. saracatinib 36-47 activin A receptor, type 1 like Danio rerio 73-77 33451301-0 2021 Post-status epilepticus treatment with the Fyn inhibitor, saracatinib, improves cognitive function in mice. saracatinib 58-69 Fyn proto-oncogene Mus musculus 43-46 33334906-7 2021 BRCA2-null prostate cancer cell lines had increased SRC phosphorylation and higher sensitivity to SRC inhibitors (eg, dasatinib, bosutinib, and saracatinib) relative to wild-type cells. saracatinib 144-155 BRCA2 DNA repair associated Homo sapiens 0-5 33175322-7 2021 Saracatinib, a nonselective Fyn inhibitor, has already been tested in clinical trials for Alzheimer"s disease, and novel selective Fyn inhibitors are under investigation. saracatinib 0-11 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 28-31 32876513-7 2021 The IGF2BP1-SRC/ERK2 axis is targetable by the SRC-inhibitor saracatinib and MEK-inhibitor selumetinib. saracatinib 61-72 insulin-like growth factor 2 mRNA binding protein 1 Mus musculus 4-11 32876513-7 2021 The IGF2BP1-SRC/ERK2 axis is targetable by the SRC-inhibitor saracatinib and MEK-inhibitor selumetinib. saracatinib 61-72 Rous sarcoma oncogene Mus musculus 12-15 32876513-7 2021 The IGF2BP1-SRC/ERK2 axis is targetable by the SRC-inhibitor saracatinib and MEK-inhibitor selumetinib. saracatinib 61-72 mitogen-activated protein kinase 1 Mus musculus 16-20 32876513-7 2021 The IGF2BP1-SRC/ERK2 axis is targetable by the SRC-inhibitor saracatinib and MEK-inhibitor selumetinib. saracatinib 61-72 Rous sarcoma oncogene Mus musculus 47-50 33451301-4 2021 Saracatinib, a Fyn inhibitor, suppresses epileptogenesis and reduces epileptiform spikes. saracatinib 0-11 Fyn proto-oncogene Mus musculus 15-18 33451301-9 2021 CONCLUSIONS: These results showed that saracatinib can improve cognitive functions by reducing the loss of hippocampal neurons after SE, suggesting that Fyn dysfunction is involved in cognitive deficits after SE, and that the inhibition of Fyn is a possible treatment to improve cognitive function in SE patients. saracatinib 39-50 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 153-156 32604782-6 2020 Upon silencing NOX2/4 gene expression and using the SRC inhibitor (AZD0530), progression of TGF-beta1 induced EMT related cellular remodeling, extra cellular matrix (ECM) production, cell migration and invasion, got significantly reverted. saracatinib 67-74 cytochrome b-245 beta chain Homo sapiens 15-21 32896567-7 2020 Furthermore, Saracatinib (Src inhibition) and BI2536 (PLK1 inhibition) diminished GSC self-renewal in vitro, and combining the two inhibitors increased survival of orthotopic tumor-bearing mice. saracatinib 13-24 Rous sarcoma oncogene Mus musculus 26-29 32692785-7 2020 We found that TBB (a casein kinase II inhibitor), AR and LiCl (GSK-3 inhibitors), cyclosporin A (calcineurin inhibitor), and Saracatinib (Fyn kinase inhibitor) caused robust inhibition of OA-induced monomeric and oligomeric p-tau in both N2a and CTX culture. saracatinib 125-136 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 138-141 32692785-7 2020 We found that TBB (a casein kinase II inhibitor), AR and LiCl (GSK-3 inhibitors), cyclosporin A (calcineurin inhibitor), and Saracatinib (Fyn kinase inhibitor) caused robust inhibition of OA-induced monomeric and oligomeric p-tau in both N2a and CTX culture. saracatinib 125-136 microtubule associated protein tau Homo sapiens 226-229 32692785-9 2020 This study provides a comprehensive view of potential drug candidates (TBB, CsA, AR, and Saracatinib), and their efficacy against tau hyperphosphorylation and oligomerization processes. saracatinib 89-100 microtubule associated protein tau Homo sapiens 130-133 32372484-7 2020 The brain-permeable c-src inhibitor, saracatinib, efficiently reduces alpha-syn propagation into neighboring regions in an in vivo model system. saracatinib 37-48 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 20-25 32372484-7 2020 The brain-permeable c-src inhibitor, saracatinib, efficiently reduces alpha-syn propagation into neighboring regions in an in vivo model system. saracatinib 37-48 synuclein alpha Homo sapiens 70-79 32635977-3 2020 Phosphorylation of Lyn, Akt, a PI3K substrate, and MAPKs including ERK, JNK, and p38, as well as the intracellular Ca2+ increase induced by this stimulation were also suppressed by saracatinib. saracatinib 181-192 LYN proto-oncogene, Src family tyrosine kinase Mus musculus 19-22 32635977-3 2020 Phosphorylation of Lyn, Akt, a PI3K substrate, and MAPKs including ERK, JNK, and p38, as well as the intracellular Ca2+ increase induced by this stimulation were also suppressed by saracatinib. saracatinib 181-192 thymoma viral proto-oncogene 1 Mus musculus 24-27 32635977-3 2020 Phosphorylation of Lyn, Akt, a PI3K substrate, and MAPKs including ERK, JNK, and p38, as well as the intracellular Ca2+ increase induced by this stimulation were also suppressed by saracatinib. saracatinib 181-192 mitogen-activated protein kinase 1 Mus musculus 67-70 32635977-3 2020 Phosphorylation of Lyn, Akt, a PI3K substrate, and MAPKs including ERK, JNK, and p38, as well as the intracellular Ca2+ increase induced by this stimulation were also suppressed by saracatinib. saracatinib 181-192 mitogen-activated protein kinase 8 Mus musculus 72-75 32635977-3 2020 Phosphorylation of Lyn, Akt, a PI3K substrate, and MAPKs including ERK, JNK, and p38, as well as the intracellular Ca2+ increase induced by this stimulation were also suppressed by saracatinib. saracatinib 181-192 mitogen-activated protein kinase 14 Mus musculus 81-84 32604782-6 2020 Upon silencing NOX2/4 gene expression and using the SRC inhibitor (AZD0530), progression of TGF-beta1 induced EMT related cellular remodeling, extra cellular matrix (ECM) production, cell migration and invasion, got significantly reverted. saracatinib 67-74 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 52-55 32604782-6 2020 Upon silencing NOX2/4 gene expression and using the SRC inhibitor (AZD0530), progression of TGF-beta1 induced EMT related cellular remodeling, extra cellular matrix (ECM) production, cell migration and invasion, got significantly reverted. saracatinib 67-74 transforming growth factor beta 1 Homo sapiens 92-101 31801023-10 2020 The chemical inhibitors for c-Src (saracatinib and dasanitib) restored GPX-1 mRNA levels and GPX-1 activity in COPD airway cells in vitro. saracatinib 35-46 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 28-33 32397949-0 2021 Biophysical and computational view on the in vitro combination between an anticancer drug, saracatinib and human serum albumin. saracatinib 91-102 albumin Homo sapiens 113-126 32397949-1 2021 Interaction behaviour of an anticancer drug, saracatinib (SCB) with human serum albumin (HSA), the major carrier protein in human blood circulation was investigated using fluorescence and absorption spectroscopy as well as computational methods. saracatinib 45-56 albumin Homo sapiens 74-87 32397949-1 2021 Interaction behaviour of an anticancer drug, saracatinib (SCB) with human serum albumin (HSA), the major carrier protein in human blood circulation was investigated using fluorescence and absorption spectroscopy as well as computational methods. saracatinib 58-61 albumin Homo sapiens 74-87 31801023-10 2020 The chemical inhibitors for c-Src (saracatinib and dasanitib) restored GPX-1 mRNA levels and GPX-1 activity in COPD airway cells in vitro. saracatinib 35-46 glutathione peroxidase 1 Homo sapiens 71-76 31801023-10 2020 The chemical inhibitors for c-Src (saracatinib and dasanitib) restored GPX-1 mRNA levels and GPX-1 activity in COPD airway cells in vitro. saracatinib 35-46 glutathione peroxidase 1 Homo sapiens 93-98 31801023-11 2020 Similarly, saracatinib prevented the loss of lung Gpx-1 expression in response to chronic smoke exposure in vivo. saracatinib 11-22 glutathione peroxidase 1 Homo sapiens 50-55 32051399-0 2020 Targeting Src family kinase member Fyn by Saracatinib attenuated liver fibrosis in vitro and in vivo. saracatinib 42-53 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 10-13 32346533-9 2020 However, the addition of the Src family inhibitor saracatinib prevented resistance to vemurafenib in CUL3KD cells and reversed RAC1 activation. saracatinib 50-61 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 29-32 32346533-9 2020 However, the addition of the Src family inhibitor saracatinib prevented resistance to vemurafenib in CUL3KD cells and reversed RAC1 activation. saracatinib 50-61 cullin 3 Homo sapiens 101-105 32346533-9 2020 However, the addition of the Src family inhibitor saracatinib prevented resistance to vemurafenib in CUL3KD cells and reversed RAC1 activation. saracatinib 50-61 Rac family small GTPase 1 Homo sapiens 127-131 32120837-6 2020 Src inhibitor Saracatinib also attenuated TAA-induced expression of type I collagen, alphaSMA, and CTGF in mouse liver tissues. saracatinib 14-25 Rous sarcoma oncogene Mus musculus 0-3 32120837-6 2020 Src inhibitor Saracatinib also attenuated TAA-induced expression of type I collagen, alphaSMA, and CTGF in mouse liver tissues. saracatinib 14-25 actin alpha 2, smooth muscle, aorta Mus musculus 85-93 32120837-6 2020 Src inhibitor Saracatinib also attenuated TAA-induced expression of type I collagen, alphaSMA, and CTGF in mouse liver tissues. saracatinib 14-25 cellular communication network factor 2 Mus musculus 99-103 31981897-6 2020 Significantly, Ectopic expression of wild-type AGO2, but not the three tyrosine site mutants, has an obvious tumor-promoting effect in vitro and in vivo, which function could be blocked thoroughly by treatment with c-Src kinase inhibitor, Saracatinib. saracatinib 239-250 argonaute RISC catalytic component 2 Homo sapiens 47-51 31981897-6 2020 Significantly, Ectopic expression of wild-type AGO2, but not the three tyrosine site mutants, has an obvious tumor-promoting effect in vitro and in vivo, which function could be blocked thoroughly by treatment with c-Src kinase inhibitor, Saracatinib. saracatinib 239-250 C-terminal Src kinase Homo sapiens 215-227 32051399-0 2020 Targeting Src family kinase member Fyn by Saracatinib attenuated liver fibrosis in vitro and in vivo. saracatinib 42-53 Fyn proto-oncogene Mus musculus 35-38 32051399-11 2020 Saracatinib treatment abolished the activation of Fyn, downregulated the Fyn/FAK/N-WASP signaling in HSCs, and subsequently prevented the activation of HSCs. saracatinib 0-11 Fyn proto-oncogene Mus musculus 50-53 32051399-11 2020 Saracatinib treatment abolished the activation of Fyn, downregulated the Fyn/FAK/N-WASP signaling in HSCs, and subsequently prevented the activation of HSCs. saracatinib 0-11 Fyn proto-oncogene Mus musculus 73-76 32051399-11 2020 Saracatinib treatment abolished the activation of Fyn, downregulated the Fyn/FAK/N-WASP signaling in HSCs, and subsequently prevented the activation of HSCs. saracatinib 0-11 PTK2 protein tyrosine kinase 2 Mus musculus 77-80 32051399-11 2020 Saracatinib treatment abolished the activation of Fyn, downregulated the Fyn/FAK/N-WASP signaling in HSCs, and subsequently prevented the activation of HSCs. saracatinib 0-11 WASP like actin nucleation promoting factor Mus musculus 81-87 32051399-12 2020 Saracatinib treatment significantly reduced the severity liver fibrosis induced by CCl4 in mice. saracatinib 0-11 chemokine (C-C motif) ligand 4 Mus musculus 83-87 32051399-15 2020 Fyn inhibitor Saracatinib significantly inhibited HSC activation and attenuated liver fibrosis in mouse model. saracatinib 14-25 Fyn proto-oncogene Mus musculus 0-3 31101744-10 2019 After treatment with saracatinib, hippocampal SUVR(WB) in APP/PS1 mice was significantly increased (P = 0.037, paired t test). saracatinib 21-32 presenilin 1 Mus musculus 62-65 31931755-12 2020 Interference with ABCG1 expression or inhibition of Wnt signaling resulted in reversal of the saracatinib-induced oxaliplatin resistance in HCC. saracatinib 94-105 ATP binding cassette subfamily G member 1 Homo sapiens 18-23 31931755-13 2020 CONCLUSIONS: These studies demonstrated that combined or sequential chemotherapy with oxaliplatin and saracatinib reduced antitumor efficacy, and this antagonism was attributed to the activation of Wnt signaling and upregulation of ABCG1 by saracatinib. saracatinib 102-113 ATP binding cassette subfamily G member 1 Homo sapiens 232-237 31931755-0 2020 Oxaliplatin resistance is enhanced by saracatinib via upregulation Wnt-ABCG1 signaling in hepatocellular carcinoma. saracatinib 38-49 ATP binding cassette subfamily G member 1 Homo sapiens 71-76 31805962-0 2019 Simultaneously inactivating Src and AKT by saracatinib/capivasertib co-delivery nanoparticles to improve the efficacy of anti-Src therapy in head and neck squamous cell carcinoma. saracatinib 43-54 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 28-31 31805962-0 2019 Simultaneously inactivating Src and AKT by saracatinib/capivasertib co-delivery nanoparticles to improve the efficacy of anti-Src therapy in head and neck squamous cell carcinoma. saracatinib 43-54 AKT serine/threonine kinase 1 Homo sapiens 36-39 31805962-0 2019 Simultaneously inactivating Src and AKT by saracatinib/capivasertib co-delivery nanoparticles to improve the efficacy of anti-Src therapy in head and neck squamous cell carcinoma. saracatinib 43-54 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 126-129 31805962-4 2019 METHODS: Dual drug-loaded nanoparticles (NPs) were developed to co-deliver Src inhibitor saracatinib (AZD0530) and AKT inhibitor capivasertib (AZD5363) into the same population of tumor cells. saracatinib 89-100 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 75-78 31805962-4 2019 METHODS: Dual drug-loaded nanoparticles (NPs) were developed to co-deliver Src inhibitor saracatinib (AZD0530) and AKT inhibitor capivasertib (AZD5363) into the same population of tumor cells. saracatinib 102-109 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 75-78 31805962-10 2019 Cathepsin B-sensitive NPs for co-delivering saracatinib and capivasertib significantly improved the efficacy of tumor repression without increasing side effects, which were due to highly specific tumor-targeting drug delivery system and synergistic anticancer effects by co-inactivation of AKT and Src in HNSCC cells. saracatinib 44-55 cathepsin B Homo sapiens 0-11 31805962-10 2019 Cathepsin B-sensitive NPs for co-delivering saracatinib and capivasertib significantly improved the efficacy of tumor repression without increasing side effects, which were due to highly specific tumor-targeting drug delivery system and synergistic anticancer effects by co-inactivation of AKT and Src in HNSCC cells. saracatinib 44-55 AKT serine/threonine kinase 1 Homo sapiens 290-293 31805962-10 2019 Cathepsin B-sensitive NPs for co-delivering saracatinib and capivasertib significantly improved the efficacy of tumor repression without increasing side effects, which were due to highly specific tumor-targeting drug delivery system and synergistic anticancer effects by co-inactivation of AKT and Src in HNSCC cells. saracatinib 44-55 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 298-301 31101744-13 2019 Conclusion: On the basis of the 11C-UCB-J PET results, hippocampal synaptic density was lower in APP/PS1 mice than in WT mice at baseline, and this deficit was normalized by treatment with saracatinib. saracatinib 189-200 presenilin 1 Mus musculus 101-104 30536923-0 2019 The Fyn kinase inhibitor, AZD0530, suppresses mouse alcohol self-administration and seeking. saracatinib 26-33 Fyn proto-oncogene Mus musculus 4-7 30536923-3 2019 Here, we used AZD0530, a CNS penetrable inhibitor of Src PTKs developed for the treatment of Alzheimer disease and cancer and tested its efficacy to suppress alcohol-dependent molecular and behavioral effects. saracatinib 14-21 Fyn proto-oncogene Mus musculus 53-56 30536923-4 2019 We show that systemic administration of AZD0530 prevents alcohol-induced Fyn activation and GluN2B phosphorylation in the DMS of mice. saracatinib 40-47 Fyn proto-oncogene Mus musculus 73-76 30536923-4 2019 We show that systemic administration of AZD0530 prevents alcohol-induced Fyn activation and GluN2B phosphorylation in the DMS of mice. saracatinib 40-47 glutamate receptor, ionotropic, NMDA2B (epsilon 2) Mus musculus 92-98 30536923-6 2019 Together, our findings suggest that AZD0530, through its inhibitory actions on Fyn kinase, dampens alcohol seeking and drinking. saracatinib 36-43 Fyn proto-oncogene Mus musculus 79-82 31667062-0 2019 An exploratory randomized-controlled trial of the efficacy of the Src-kinase inhibitor saracatinib as a novel analgesic for cancer-induced bone pain. saracatinib 87-98 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 66-69 31416844-6 2019 However, we show that the SRC inhibitor, saracatinib, can block the DBL-driven resistance. saracatinib 41-52 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 26-29 31416844-6 2019 However, we show that the SRC inhibitor, saracatinib, can block the DBL-driven resistance. saracatinib 41-52 MCF.2 cell line derived transforming sequence Homo sapiens 68-71 31329216-2 2019 AZD0530 is an investigational kinase inhibitor specific for the Src family, including fyn, that has been repurposed for the treatment of Alzheimer disease. saracatinib 0-7 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 64-67 31329216-2 2019 AZD0530 is an investigational kinase inhibitor specific for the Src family, including fyn, that has been repurposed for the treatment of Alzheimer disease. saracatinib 0-7 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 86-89 31667062-3 2019 The non-receptor tyrosine kinase Src is thought to act as a hub for regulating NMDA receptor activity and the orally available Src inhibitor saracatinib has shown promise as a potential analgesic in recent animal studies. saracatinib 141-152 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 127-130 30504771-7 2018 Pharmaceutical intervention with AZD0530 markedly reverses LIF-mediated cancer dissemination and local invasion through promotion of cytoplasmic accumulation of YAP1 and suppression of focal adhesion kinases. saracatinib 33-40 Yes1 associated transcriptional regulator Homo sapiens 161-165 30628679-10 2019 However, blocking Src activity with saracatinib prevented CX3CL1-mediated cell migration and invasion. saracatinib 36-47 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 18-21 30628679-10 2019 However, blocking Src activity with saracatinib prevented CX3CL1-mediated cell migration and invasion. saracatinib 36-47 C-X3-C motif chemokine ligand 1 Homo sapiens 58-64 30207834-5 2019 SRC pathway inhibition by Saracatinib resulted in reduced TLK2-mediated glioblastoma migration, invasion, confirming a key role for SRC signaling in regulating the functions of TLK2. saracatinib 26-37 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 0-3 30207834-5 2019 SRC pathway inhibition by Saracatinib resulted in reduced TLK2-mediated glioblastoma migration, invasion, confirming a key role for SRC signaling in regulating the functions of TLK2. saracatinib 26-37 tousled like kinase 2 Homo sapiens 58-62 30207834-5 2019 SRC pathway inhibition by Saracatinib resulted in reduced TLK2-mediated glioblastoma migration, invasion, confirming a key role for SRC signaling in regulating the functions of TLK2. saracatinib 26-37 tousled like kinase 2 Homo sapiens 177-181 30817315-5 2019 Mechanism studies revealed that the induction of SAA1 expression by cortisol and SAA1 was blocked by either the transcription factor STAT3 antagonist AZD0530 or siRNA-mediated knockdown of STAT3. saracatinib 150-157 serum amyloid A1 Homo sapiens 49-53 30817315-5 2019 Mechanism studies revealed that the induction of SAA1 expression by cortisol and SAA1 was blocked by either the transcription factor STAT3 antagonist AZD0530 or siRNA-mediated knockdown of STAT3. saracatinib 150-157 serum amyloid A1 Homo sapiens 81-85 30817315-5 2019 Mechanism studies revealed that the induction of SAA1 expression by cortisol and SAA1 was blocked by either the transcription factor STAT3 antagonist AZD0530 or siRNA-mediated knockdown of STAT3. saracatinib 150-157 signal transducer and activator of transcription 3 Homo sapiens 133-138 30166523-10 2018 A Src inhibitor saracatinib sensitized esophageal cancer cells to irradiation. saracatinib 16-27 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 2-5 29959144-6 2018 Treatment of established lines and primary ovarian cancer cultures with Src and MEK inhibitors saracatinib and selumetinib, respectively, showed target kinase inhibition and synergistic induction of apoptosis and cell-cycle arrest in vitro, and tumor inhibition in xenografts. saracatinib 95-106 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 72-75 29959144-6 2018 Treatment of established lines and primary ovarian cancer cultures with Src and MEK inhibitors saracatinib and selumetinib, respectively, showed target kinase inhibition and synergistic induction of apoptosis and cell-cycle arrest in vitro, and tumor inhibition in xenografts. saracatinib 95-106 mitogen-activated protein kinase kinase 7 Homo sapiens 80-83 29530864-5 2018 Astonishingly, the transport efficiencies (TEs) of ETT for saracatinib and some nucleoside drugs were as high as the TE for ET. saracatinib 59-70 solute carrier family 22 member 4 Homo sapiens 51-54 29555825-10 2018 Fyn inhibitors AZD0530 and PP1 significantly attenuated OA progression by blocking the beta-catenin pathway and reducing the levels of extracellular matrix catabolic enzymes in the articular cartilage. saracatinib 15-22 Fyn proto-oncogene Mus musculus 0-3 29555825-10 2018 Fyn inhibitors AZD0530 and PP1 significantly attenuated OA progression by blocking the beta-catenin pathway and reducing the levels of extracellular matrix catabolic enzymes in the articular cartilage. saracatinib 15-22 catenin (cadherin associated protein), beta 1 Mus musculus 87-99 29401603-10 2018 HBc-induced cellular proliferation and tumor formation were reversed by administration of the Src inhibitor saracatinib. saracatinib 108-119 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 94-97 29925404-10 2018 Mechanistic assessment of the drug effects in HNSCC cells showed that saracatinib induced suppression of Src-dependent invasion/metastasis through downregulating the expression levels of Vimentin and Snail proteins. saracatinib 70-81 vimentin Mus musculus 187-195 29925404-10 2018 Mechanistic assessment of the drug effects in HNSCC cells showed that saracatinib induced suppression of Src-dependent invasion/metastasis through downregulating the expression levels of Vimentin and Snail proteins. saracatinib 70-81 snail family zinc finger 1 Mus musculus 200-205 29601121-4 2018 In our study, we established an Src inhibitor saracatinib-resistant breast cancer cell line (SKBR-3/SI) for the first time and by evaluating mRNA expression profile, we found that plasminogen activator inhibitor-1 (PAI-1) was upregulated in saracatinib-resistant cells compared to the parent cells. saracatinib 46-57 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 32-35 29601121-4 2018 In our study, we established an Src inhibitor saracatinib-resistant breast cancer cell line (SKBR-3/SI) for the first time and by evaluating mRNA expression profile, we found that plasminogen activator inhibitor-1 (PAI-1) was upregulated in saracatinib-resistant cells compared to the parent cells. saracatinib 46-57 serpin family E member 1 Homo sapiens 180-213 29601121-4 2018 In our study, we established an Src inhibitor saracatinib-resistant breast cancer cell line (SKBR-3/SI) for the first time and by evaluating mRNA expression profile, we found that plasminogen activator inhibitor-1 (PAI-1) was upregulated in saracatinib-resistant cells compared to the parent cells. saracatinib 46-57 serpin family E member 1 Homo sapiens 215-220 29601121-4 2018 In our study, we established an Src inhibitor saracatinib-resistant breast cancer cell line (SKBR-3/SI) for the first time and by evaluating mRNA expression profile, we found that plasminogen activator inhibitor-1 (PAI-1) was upregulated in saracatinib-resistant cells compared to the parent cells. saracatinib 241-252 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 32-35 29601121-4 2018 In our study, we established an Src inhibitor saracatinib-resistant breast cancer cell line (SKBR-3/SI) for the first time and by evaluating mRNA expression profile, we found that plasminogen activator inhibitor-1 (PAI-1) was upregulated in saracatinib-resistant cells compared to the parent cells. saracatinib 241-252 serpin family E member 1 Homo sapiens 180-213 29601121-4 2018 In our study, we established an Src inhibitor saracatinib-resistant breast cancer cell line (SKBR-3/SI) for the first time and by evaluating mRNA expression profile, we found that plasminogen activator inhibitor-1 (PAI-1) was upregulated in saracatinib-resistant cells compared to the parent cells. saracatinib 241-252 serpin family E member 1 Homo sapiens 215-220 29601121-5 2018 Further study demonstrated that PAI-1 might induce saracatinib resistance in breast cancer cells by increasing the secretion of chemokine (C-C motif) ligand 5 (CCL5). saracatinib 51-62 serpin family E member 1 Homo sapiens 32-37 29601121-5 2018 Further study demonstrated that PAI-1 might induce saracatinib resistance in breast cancer cells by increasing the secretion of chemokine (C-C motif) ligand 5 (CCL5). saracatinib 51-62 C-C motif chemokine ligand 5 Homo sapiens 128-158 29601121-5 2018 Further study demonstrated that PAI-1 might induce saracatinib resistance in breast cancer cells by increasing the secretion of chemokine (C-C motif) ligand 5 (CCL5). saracatinib 51-62 C-C motif chemokine ligand 5 Homo sapiens 160-164 29601121-6 2018 Functional assays showed that PAI-1 and CCL5 overexpression promoted cell proliferation and migration in breast cancer cells, while inhibition of PAI-1 and CCL5 decreased cell proliferation and migration in saracatinib-resistant cells. saracatinib 207-218 serpin family E member 1 Homo sapiens 146-151 29601121-6 2018 Functional assays showed that PAI-1 and CCL5 overexpression promoted cell proliferation and migration in breast cancer cells, while inhibition of PAI-1 and CCL5 decreased cell proliferation and migration in saracatinib-resistant cells. saracatinib 207-218 C-C motif chemokine ligand 5 Homo sapiens 156-160 29601121-7 2018 We also showed that targeting PAI-1 or CCL5 could reverse saracatinib resistance, which deserves more attention in clinical settings. saracatinib 58-69 serpin family E member 1 Homo sapiens 30-35 29601121-7 2018 We also showed that targeting PAI-1 or CCL5 could reverse saracatinib resistance, which deserves more attention in clinical settings. saracatinib 58-69 C-C motif chemokine ligand 5 Homo sapiens 39-43 29435137-4 2018 Using two complementary strategies; a targeted tumour suppressor gene siRNA screen, and a phospho-receptor tyrosine kinase array, we demonstrate that activation of MAPK signalling, via a reduction in NF1 (neurofibromin) expression or overexpression of HER2 and the insulin receptor, can drive resistance to AZD0530. saracatinib 307-314 mitogen-activated protein kinase 1 Homo sapiens 164-168 28840468-9 2018 Pre-administration of saracatinib (AZD0530), an inhibitor of Fyn activity, also significantly reduced LID in dyskinetic wild-type mice. saracatinib 22-33 Fyn proto-oncogene Mus musculus 61-64 28840468-9 2018 Pre-administration of saracatinib (AZD0530), an inhibitor of Fyn activity, also significantly reduced LID in dyskinetic wild-type mice. saracatinib 35-42 Fyn proto-oncogene Mus musculus 61-64 29550144-0 2018 miR-19b-3p inhibits breast cancer cell proliferation and reverses saracatinib-resistance by regulating PI3K/Akt pathway. saracatinib 66-77 microRNA 19b-1 Homo sapiens 0-7 29550144-0 2018 miR-19b-3p inhibits breast cancer cell proliferation and reverses saracatinib-resistance by regulating PI3K/Akt pathway. saracatinib 66-77 AKT serine/threonine kinase 1 Homo sapiens 108-111 29550144-6 2018 In this study, we established a Src inhibitor saracatinib-resistant breast cancer cell line (SK-BR-3/SI) for the first time. saracatinib 46-57 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 32-35 29550144-7 2018 Microarray data and qRT-PCR results showed that miR-19b-3p expression was downregulated in saracatinib-resistant cells compared with saracatinib-sensitive cells. saracatinib 91-102 microRNA 19b-1 Homo sapiens 48-55 29550144-7 2018 Microarray data and qRT-PCR results showed that miR-19b-3p expression was downregulated in saracatinib-resistant cells compared with saracatinib-sensitive cells. saracatinib 133-144 microRNA 19b-1 Homo sapiens 48-55 29550144-8 2018 Downregulation of miR-19b-3p remarkably increased the IC50 value of saracatinib, and promoted cell migration. saracatinib 68-79 microRNA 19b-1 Homo sapiens 18-25 29191754-2 2018 Because no investigational agents have demonstrated disease-modifying effects clinically, we tested whether the Fyn inhibitor, saracatinib, provides persistent improvement in a transgenic model. saracatinib 127-138 Fyn proto-oncogene Mus musculus 112-115 29535838-8 2018 Dasatinib and saracatinib have potent inhibitory effects on Yes and treatment with either resulted in downregulation of YAP1 transcription targets, reduced cell viability, and G0-G1 cell cycle arrest. saracatinib 14-25 Yes1 associated transcriptional regulator Homo sapiens 120-124 29435137-0 2018 Activation of MAPK signalling results in resistance to saracatinib (AZD0530) in ovarian cancer. saracatinib 55-66 mitogen-activated protein kinase 1 Homo sapiens 14-18 29435137-0 2018 Activation of MAPK signalling results in resistance to saracatinib (AZD0530) in ovarian cancer. saracatinib 68-75 mitogen-activated protein kinase 1 Homo sapiens 14-18 29435137-2 2018 The SAPPROC trial investigated the addition of the SRC inhibitor saracatinib (AZD0530) to weekly paclitaxel for the treatment of platinum resistant ovarian cancer; however, this drug combination did not provide any benefit to progression free survival (PFS) of women with platinum resistant disease. saracatinib 65-76 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 51-54 29435137-2 2018 The SAPPROC trial investigated the addition of the SRC inhibitor saracatinib (AZD0530) to weekly paclitaxel for the treatment of platinum resistant ovarian cancer; however, this drug combination did not provide any benefit to progression free survival (PFS) of women with platinum resistant disease. saracatinib 78-85 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 51-54 29435137-5 2018 Knockdown of NF1 in two ovarian cancer cell lines resulted in resistance to AZD0530, and was accompanied with activated MEK and ERK signalling. saracatinib 76-83 neurofibromin 1 Homo sapiens 13-16 29435137-6 2018 We also show that silencing of HER2 and the insulin receptor can partially resensitize AZD0530 resistant cells, which was associated with decreased phosphorylation of MEK and ERK. saracatinib 87-94 erb-b2 receptor tyrosine kinase 2 Homo sapiens 31-35 29435137-6 2018 We also show that silencing of HER2 and the insulin receptor can partially resensitize AZD0530 resistant cells, which was associated with decreased phosphorylation of MEK and ERK. saracatinib 87-94 insulin receptor Homo sapiens 44-60 29435137-6 2018 We also show that silencing of HER2 and the insulin receptor can partially resensitize AZD0530 resistant cells, which was associated with decreased phosphorylation of MEK and ERK. saracatinib 87-94 mitogen-activated protein kinase kinase 7 Homo sapiens 167-170 29435137-6 2018 We also show that silencing of HER2 and the insulin receptor can partially resensitize AZD0530 resistant cells, which was associated with decreased phosphorylation of MEK and ERK. saracatinib 87-94 mitogen-activated protein kinase 1 Homo sapiens 175-178 29435137-7 2018 Furthermore, we demonstrate a synergistic effect of combining SRC and MEK inhibitors in both AZD0530 sensitive and resistant cells, and that MEK inhibition is sufficient to completely resensitize AZD0530 resistant cells. saracatinib 93-100 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 62-65 29435137-7 2018 Furthermore, we demonstrate a synergistic effect of combining SRC and MEK inhibitors in both AZD0530 sensitive and resistant cells, and that MEK inhibition is sufficient to completely resensitize AZD0530 resistant cells. saracatinib 93-100 mitogen-activated protein kinase kinase 7 Homo sapiens 70-73 29435137-7 2018 Furthermore, we demonstrate a synergistic effect of combining SRC and MEK inhibitors in both AZD0530 sensitive and resistant cells, and that MEK inhibition is sufficient to completely resensitize AZD0530 resistant cells. saracatinib 196-203 mitogen-activated protein kinase kinase 7 Homo sapiens 141-144 29021139-5 2017 Inhibition of Pxn phosphorylation by the Src inhibitor saracatinib or its knockdown via shRNA dramatically altered adhesion and spreading of freshly isolated CD8+/CD103+ lung tumor-infiltrating lymphocytes and CD103+ tumor-specific CTL clones. saracatinib 55-66 paxillin Homo sapiens 14-17 29021139-5 2017 Inhibition of Pxn phosphorylation by the Src inhibitor saracatinib or its knockdown via shRNA dramatically altered adhesion and spreading of freshly isolated CD8+/CD103+ lung tumor-infiltrating lymphocytes and CD103+ tumor-specific CTL clones. saracatinib 55-66 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 41-44 29021139-5 2017 Inhibition of Pxn phosphorylation by the Src inhibitor saracatinib or its knockdown via shRNA dramatically altered adhesion and spreading of freshly isolated CD8+/CD103+ lung tumor-infiltrating lymphocytes and CD103+ tumor-specific CTL clones. saracatinib 55-66 CD8a molecule Homo sapiens 158-161 29021139-5 2017 Inhibition of Pxn phosphorylation by the Src inhibitor saracatinib or its knockdown via shRNA dramatically altered adhesion and spreading of freshly isolated CD8+/CD103+ lung tumor-infiltrating lymphocytes and CD103+ tumor-specific CTL clones. saracatinib 55-66 integrin subunit alpha E Homo sapiens 163-168 29021139-5 2017 Inhibition of Pxn phosphorylation by the Src inhibitor saracatinib or its knockdown via shRNA dramatically altered adhesion and spreading of freshly isolated CD8+/CD103+ lung tumor-infiltrating lymphocytes and CD103+ tumor-specific CTL clones. saracatinib 55-66 integrin subunit alpha E Homo sapiens 210-215 29021139-6 2017 Inhibition of Pxn phosphorylation with saracatinib in these CTL clones also severely compromised their functional activities toward autologous tumor cells. saracatinib 39-50 paxillin Homo sapiens 14-17 28818835-5 2017 The intracerebroventricular or stereotaxic injection of a Src inhibitor (AZD0530), or Src shRNA viruses attenuated pY336 levels, and several somatic withdrawal signs. saracatinib 73-80 Rous sarcoma oncogene Mus musculus 58-61 28116540-9 2017 Inhibition of SRC by Saracatinib (SARC) blocked GDNF function and accelerated TZMB-mediated cell death in TSTC, but GDNF continued promoting TRTC growth. saracatinib 21-32 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 28775147-5 2017 We demonstrated that merlin-deficient mouse Schwann cells (MD-MSC) treated with the c-Met inhibitor, cabozantinib, or the Src kinase inhibitors, dasatinib and saracatinib, underwent a G1 cell-cycle arrest. saracatinib 159-170 neurofibromin 2 Mus musculus 21-27 28775147-5 2017 We demonstrated that merlin-deficient mouse Schwann cells (MD-MSC) treated with the c-Met inhibitor, cabozantinib, or the Src kinase inhibitors, dasatinib and saracatinib, underwent a G1 cell-cycle arrest. saracatinib 159-170 Rous sarcoma oncogene Mus musculus 122-125 28775147-8 2017 Moreover, human vestibular schwannoma cells with NF2 mutations had a 40% decrease in cell viability when treated with cabozantinib and saracatinib together compared with the vehicle control. saracatinib 135-146 NF2, moesin-ezrin-radixin like (MERLIN) tumor suppressor Homo sapiens 49-52 29066500-9 2017 We demonstrated that tumor outgrowth from PTPN23-deficient BT474 cells was suppressed in a xenograft model in vivo upon treatment with AZD0530, an SFK inhibitor. saracatinib 135-142 protein tyrosine phosphatase non-receptor type 23 Homo sapiens 42-48 28838952-5 2017 Targeting LCK signaling via saracatinib, an inhibitor currently undergoing clinical evaluation, sensitized chemoresistant cells to cisplatin. saracatinib 28-39 LCK proto-oncogene, Src family tyrosine kinase Homo sapiens 10-13 28455521-0 2017 Importance of the novel organic cation transporter 1 for tyrosine kinase inhibition by saracatinib in rheumatoid arthritis synovial fibroblasts. saracatinib 87-98 TXK tyrosine kinase Homo sapiens 57-72 28455521-3 2017 Since intracellular effective TKIs must enter the cell to reach their intracellular targets, here we investigated the interaction of the TKI saracatinib, a dual inhibitor of c-Src and c-Abl signaling, with transporters for organic cations as well as the role of these transporters for the biological effect of saracatinib in human RA-synovial fibroblasts (hRASF). saracatinib 141-152 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 174-179 28455521-3 2017 Since intracellular effective TKIs must enter the cell to reach their intracellular targets, here we investigated the interaction of the TKI saracatinib, a dual inhibitor of c-Src and c-Abl signaling, with transporters for organic cations as well as the role of these transporters for the biological effect of saracatinib in human RA-synovial fibroblasts (hRASF). saracatinib 141-152 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 184-189 28455521-5 2017 The cellular saracatinib uptake was mainly dependent on the human novel organic cation transporter 1 (hOCTN1), which showed the highest apparent affinity for saracatinib among all other transporters for organic cations analyzed here. saracatinib 13-24 solute carrier family 22 member 4 Homo sapiens 102-108 28455521-5 2017 The cellular saracatinib uptake was mainly dependent on the human novel organic cation transporter 1 (hOCTN1), which showed the highest apparent affinity for saracatinib among all other transporters for organic cations analyzed here. saracatinib 158-169 solute carrier family 22 member 4 Homo sapiens 102-108 28455521-6 2017 In hRASF, saracatinib biologic function was dependent on hOCTN1. saracatinib 10-21 solute carrier family 22 member 4 Homo sapiens 57-63 28455521-7 2017 Further analysis showed that disease specific factors (pH, inflammatory cytokines such as TNFalpha) regulated saracatinib uptake in hRASF. saracatinib 110-121 tumor necrosis factor Homo sapiens 90-98 28561330-21 2017 In old arteries, Src inhibition (saracatinib) increased: (i) 140 kDa VE-cadherin in the TTX-insoluble fraction, (ii) VE-cadherin intensity at AJs, (iii) AJ width, and (iv) acetylcholine dilatation. saracatinib 33-44 SRC proto-oncogene, non-receptor tyrosine kinase Rattus norvegicus 17-20 28561330-21 2017 In old arteries, Src inhibition (saracatinib) increased: (i) 140 kDa VE-cadherin in the TTX-insoluble fraction, (ii) VE-cadherin intensity at AJs, (iii) AJ width, and (iv) acetylcholine dilatation. saracatinib 33-44 cadherin 5 Rattus norvegicus 69-80 28561330-21 2017 In old arteries, Src inhibition (saracatinib) increased: (i) 140 kDa VE-cadherin in the TTX-insoluble fraction, (ii) VE-cadherin intensity at AJs, (iii) AJ width, and (iv) acetylcholine dilatation. saracatinib 33-44 cadherin 5 Rattus norvegicus 117-128 28116540-9 2017 Inhibition of SRC by Saracatinib (SARC) blocked GDNF function and accelerated TZMB-mediated cell death in TSTC, but GDNF continued promoting TRTC growth. saracatinib 21-32 glial cell derived neurotrophic factor Homo sapiens 48-52 28396832-0 2017 AZD0530 sensitizes drug-resistant ALK-positive lung cancer cells by inhibiting SRC signaling. saracatinib 0-7 ALK receptor tyrosine kinase Homo sapiens 34-37 28396832-0 2017 AZD0530 sensitizes drug-resistant ALK-positive lung cancer cells by inhibiting SRC signaling. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 79-82 28396832-5 2017 Furthermore, SRC inhibition by AZD0530 was effective in ALK-resistant cancer cells. saracatinib 31-38 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 13-16 28396832-5 2017 Furthermore, SRC inhibition by AZD0530 was effective in ALK-resistant cancer cells. saracatinib 31-38 ALK receptor tyrosine kinase Homo sapiens 56-59 28396832-6 2017 Thus, ALK inhibition by ceritinib may lead to upregulation of SRC signaling, and AZD0530 could serve as a potential drug in the clinic to treat ALK-resistant lung cancer patients. saracatinib 81-88 ALK receptor tyrosine kinase Homo sapiens 144-147 27460949-5 2016 Phosphorylation level of Src pathway signalling molecules, such as Src, FAK and Stat3, were also reduced in vitro and in vivo, as a result of the anti-metastasic effects caused by saracatinib treatment. saracatinib 180-191 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 25-28 28049762-7 2017 Pharmacological inhibition of Src with AZD0530 and clustered regularly interspaced short palindromic repeats/Cas9-mediated knockout of Src demonstrated that Src was critical for activating the TBK1-IRF3 pathway and stimulating type I IFN production. saracatinib 39-46 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 30-33 27766744-0 2016 PTTG1 Levels Are Predictive of Saracatinib Sensitivity in Ovarian Cancer Cell Lines. saracatinib 31-42 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 0-5 27766744-3 2016 We explored the sensitivity of ovarian cancer cell lines to the Src kinase inhibitor saracatinib to identify predictive markers of drug sensitivity using gene microarrays. saracatinib 85-96 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 64-67 27766744-4 2016 Pituitary tumor transforming gene 1 (PTTG1) was selected as a potential biomarker as mRNA levels were correlated with saracatinib resistance, as well as higher PTTG1 protein expression. saracatinib 118-129 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 0-35 27766744-4 2016 Pituitary tumor transforming gene 1 (PTTG1) was selected as a potential biomarker as mRNA levels were correlated with saracatinib resistance, as well as higher PTTG1 protein expression. saracatinib 118-129 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 37-42 27766744-6 2016 In sensitive cell lines, saracatinib treatment decreased PTTG1 and fibroblast growth factor 2 (FGF2) protein levels. saracatinib 25-36 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 57-62 27766744-6 2016 In sensitive cell lines, saracatinib treatment decreased PTTG1 and fibroblast growth factor 2 (FGF2) protein levels. saracatinib 25-36 fibroblast growth factor 2 Homo sapiens 67-93 27766744-6 2016 In sensitive cell lines, saracatinib treatment decreased PTTG1 and fibroblast growth factor 2 (FGF2) protein levels. saracatinib 25-36 fibroblast growth factor 2 Homo sapiens 95-99 27766744-7 2016 Downregulating PTTG1 by siRNAs increased saracatinib sensitivity in two resistant cell lines. saracatinib 41-52 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 15-20 27766744-8 2016 Our results indicate PTTG1 may be a valuable biomarker in ovarian cancer to predict sensitivity to saracatinib, and could form the basis of a targeted prospective saracatinib trial for ovarian cancer. saracatinib 99-110 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 21-26 27766744-8 2016 Our results indicate PTTG1 may be a valuable biomarker in ovarian cancer to predict sensitivity to saracatinib, and could form the basis of a targeted prospective saracatinib trial for ovarian cancer. saracatinib 163-174 PTTG1 regulator of sister chromatid separation, securin Homo sapiens 21-26 28036386-5 2016 Inhibition of src by both saracatinib (AZD0530) and siRNA could partially reverse gemcitabine resistance and attenuate resistance-associated anti-apoptosis, migration and stem cell capacities. saracatinib 26-37 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 28036386-5 2016 Inhibition of src by both saracatinib (AZD0530) and siRNA could partially reverse gemcitabine resistance and attenuate resistance-associated anti-apoptosis, migration and stem cell capacities. saracatinib 39-46 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 27666484-0 2016 Combined SRC inhibitor saracatinib and anti-ErbB2 antibody H2-18 produces a synergistic antitumor effect on trastuzumab-resistant breast cancer. saracatinib 23-34 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 9-12 27666484-3 2016 Recently, Src inhibitor saracatinib has drawn great attention for its key role in trastuzumab response. saracatinib 24-35 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 10-13 27666484-8 2016 H2-18 plus saracatinib showed a significantly more potent PCD-inducing activity compared with either H2-18 or saracatinib alone. saracatinib 110-121 sphingosine-1-phosphate receptor 2 Homo sapiens 0-5 27475932-4 2016 The present study provides preclinical evidence that Delta16HER2 expression confers de novo resistance to standard anti-HER2-therapies such as Lapatinib and acquired resistance to the selective Src inhibitor Saracatinib in breast cancer. saracatinib 208-219 erb-b2 receptor tyrosine kinase 2 Homo sapiens 60-64 27475932-4 2016 The present study provides preclinical evidence that Delta16HER2 expression confers de novo resistance to standard anti-HER2-therapies such as Lapatinib and acquired resistance to the selective Src inhibitor Saracatinib in breast cancer. saracatinib 208-219 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 194-197 27460949-5 2016 Phosphorylation level of Src pathway signalling molecules, such as Src, FAK and Stat3, were also reduced in vitro and in vivo, as a result of the anti-metastasic effects caused by saracatinib treatment. saracatinib 180-191 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 67-70 27460949-5 2016 Phosphorylation level of Src pathway signalling molecules, such as Src, FAK and Stat3, were also reduced in vitro and in vivo, as a result of the anti-metastasic effects caused by saracatinib treatment. saracatinib 180-191 protein tyrosine kinase 2 Homo sapiens 72-75 27460949-5 2016 Phosphorylation level of Src pathway signalling molecules, such as Src, FAK and Stat3, were also reduced in vitro and in vivo, as a result of the anti-metastasic effects caused by saracatinib treatment. saracatinib 180-191 signal transducer and activator of transcription 3 Homo sapiens 80-85 26941850-7 2016 In our study, Src kinase activity in cultured cells and tumor xenografts was monitored quantitatively and dynamically in response to clinical small-molecular kinase inhibitors, dasatinib and saracatinib. saracatinib 191-202 Rous sarcoma oncogene Mus musculus 14-17 27095574-0 2016 SRC kinase inhibition with saracatinib limits the development of osteolytic bone disease in multiple myeloma. saracatinib 27-38 Rous sarcoma oncogene Mus musculus 0-3 27095574-3 2016 In the current study, we investigated the effect of treatment with the SRC inhibitor saracatinib (AZD0530) on osteoclast and osteoblast differentiation and function, and on the development of MM and its associated bone disease in the 5TGM.1 and 5T2MM murine MM models. saracatinib 85-96 Rous sarcoma oncogene Mus musculus 71-74 27095574-3 2016 In the current study, we investigated the effect of treatment with the SRC inhibitor saracatinib (AZD0530) on osteoclast and osteoblast differentiation and function, and on the development of MM and its associated bone disease in the 5TGM.1 and 5T2MM murine MM models. saracatinib 98-105 Rous sarcoma oncogene Mus musculus 71-74 27094550-7 2016 We have tested this hypothesis using an orally bioavailable Src inhibitor (saracatinib) in a rat model of cancer-induced bone pain. saracatinib 75-86 SRC proto-oncogene, non-receptor tyrosine kinase Rattus norvegicus 60-63 27094550-10 2016 The analgesic mechanisms of saracatinib appear to be due to an effect on the nervous system as immunoblotting of L2-5 spinal segments showed that mammary rat metastasis tumor cells-1 injection induced phosphorylation of the GluN1 subunit of the N-methyl-D-aspartate receptor, indicative of receptor activation, and this was reduced by saracatinib. saracatinib 28-39 glutamate ionotropic receptor NMDA type subunit 1 Rattus norvegicus 224-229 27094550-10 2016 The analgesic mechanisms of saracatinib appear to be due to an effect on the nervous system as immunoblotting of L2-5 spinal segments showed that mammary rat metastasis tumor cells-1 injection induced phosphorylation of the GluN1 subunit of the N-methyl-D-aspartate receptor, indicative of receptor activation, and this was reduced by saracatinib. saracatinib 335-346 glutamate ionotropic receptor NMDA type subunit 1 Rattus norvegicus 224-229 26474384-6 2015 Complete inhibition of T24 aggregate dispersal, however, is not achieved with any single agent, although partial inhibition was observed with 10 muM of the Src inhibitor, AZD-0530. saracatinib 171-179 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 156-159 26493492-2 2016 Saracatinib potently inhibits Fyn activation. saracatinib 0-11 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 30-33 26383165-4 2015 Src kinase blockade with the small-molecule inhibitor saracatinib prevented the disorganized three-dimensional growth of ER(-) mammary epithelial cells in vitro and delayed the development of premalignant lesions and tumors in vivo in mouse models developing HER2(+) and ER(-) mammary tumors, extending tumor-free and overall survival. saracatinib 54-65 Rous sarcoma oncogene Mus musculus 0-3 26383165-4 2015 Src kinase blockade with the small-molecule inhibitor saracatinib prevented the disorganized three-dimensional growth of ER(-) mammary epithelial cells in vitro and delayed the development of premalignant lesions and tumors in vivo in mouse models developing HER2(+) and ER(-) mammary tumors, extending tumor-free and overall survival. saracatinib 54-65 erb-b2 receptor tyrosine kinase 2 Mus musculus 259-263 26045172-8 2015 Furthermore, the Src inhibitor saracatinib effectively blocked AOPP-induced phosphorylation of Src, activation of ER stress, hypertrophy, and EMT in HK-2 cells. saracatinib 31-42 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 17-20 26208525-8 2015 Saracatinib, an src kinase inhibitor, suppressed ERK1/2 phosphorylation and growth of LC-2/ad DR cells. saracatinib 0-11 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 16-19 26208525-8 2015 Saracatinib, an src kinase inhibitor, suppressed ERK1/2 phosphorylation and growth of LC-2/ad DR cells. saracatinib 0-11 mitogen-activated protein kinase 3 Homo sapiens 49-55 26325669-3 2015 To better define the molecular targets of the Src TKIs saracatinib, dasatinib and bosutinib, we used a variety of in vitro/in vivo studies. saracatinib 55-66 Rous sarcoma oncogene Mus musculus 46-49 26325669-5 2015 However, in live cells only saracatinib efficiently reduced EGFR activation, while dasatinib was the most effective agent in inhibiting Src TK. saracatinib 28-39 epidermal growth factor receptor Mus musculus 60-64 26325669-7 2015 We then identified the most effective drug combinations to overcome resistance to EGFR inhibitors, both in vitro and in nude mice: in T790M EGFR erlotinib-resistant cells, saracatinib with the anti-EGFR mAb cetuximab; in Ras mutant erlotinib-resistant models, dasatinib with the MEK inhibitor selumetinib. saracatinib 172-183 epidermal growth factor receptor Mus musculus 82-86 26325669-7 2015 We then identified the most effective drug combinations to overcome resistance to EGFR inhibitors, both in vitro and in nude mice: in T790M EGFR erlotinib-resistant cells, saracatinib with the anti-EGFR mAb cetuximab; in Ras mutant erlotinib-resistant models, dasatinib with the MEK inhibitor selumetinib. saracatinib 172-183 epidermal growth factor receptor Mus musculus 140-144 26325669-7 2015 We then identified the most effective drug combinations to overcome resistance to EGFR inhibitors, both in vitro and in nude mice: in T790M EGFR erlotinib-resistant cells, saracatinib with the anti-EGFR mAb cetuximab; in Ras mutant erlotinib-resistant models, dasatinib with the MEK inhibitor selumetinib. saracatinib 172-183 epidermal growth factor receptor Mus musculus 140-144 26045172-8 2015 Furthermore, the Src inhibitor saracatinib effectively blocked AOPP-induced phosphorylation of Src, activation of ER stress, hypertrophy, and EMT in HK-2 cells. saracatinib 31-42 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 95-98 26357463-10 2015 Src inhibitors, including PP2, PP1, Saracatinib, and Quercetin, partially inhibited LPS-induced phosphorylation of Cav-1. saracatinib 36-47 SRC proto-oncogene, non-receptor tyrosine kinase Rattus norvegicus 0-3 26357463-10 2015 Src inhibitors, including PP2, PP1, Saracatinib, and Quercetin, partially inhibited LPS-induced phosphorylation of Cav-1. saracatinib 36-47 caveolin 1 Rattus norvegicus 115-120 26062928-3 2015 Saracatinib (AZD0530) is a novel selective oral Src kinase inhibitor. saracatinib 0-11 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 48-51 26062928-3 2015 Saracatinib (AZD0530) is a novel selective oral Src kinase inhibitor. saracatinib 13-20 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 48-51 26062928-15 2015 CONCLUSION: Saracatinib is a novel oral Src kinase inhibitor that was well tolerated but failed to meet its primary endpoint of improvement in 4 month progression-free survival as a single agent in previously treated metastatic colorectal cancer patients. saracatinib 12-23 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 40-43 26009269-0 2015 A phase II study of saracatinib (AZD0530), a Src inhibitor, administered orally daily to patients with advanced thymic malignancies. saracatinib 20-31 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 45-48 25820822-10 2015 Treatment of lung cancer cells with Src inhibitor saracatinib abrogates AFB1-induced IRS2 accumulation. saracatinib 50-61 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 36-39 25820822-10 2015 Treatment of lung cancer cells with Src inhibitor saracatinib abrogates AFB1-induced IRS2 accumulation. saracatinib 50-61 insulin receptor substrate 2 Homo sapiens 85-89 26170970-10 2015 Furthermore, the Src inhibitor, saracatinib, is currently in clinical trials for the treatment of a variety of solid tumors, including breast and lung cancers. saracatinib 32-43 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 17-20 26009269-2 2015 Src plays a role in normal thymic epithelial maturation, and its inhibition with the oral compound saracatinib was postulated to be effective in controlling thymic malignancy. saracatinib 99-110 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 0-3 26009269-12 2015 CONCLUSION: Src inhibition by saracatinib did not produce any radiographic responses, though some patients did experience stable disease. saracatinib 30-41 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 12-15 25874001-5 2015 Herein, we present a Phase Ib trial of the repurposed investigational drug AZD0530, a Src family kinase inhibitor specific for Fyn and Src kinase, for the treatment of patients with mild-to-moderate AD. saracatinib 75-82 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 86-89 25707991-9 2015 RESULTS: AZD0530 potently inhibits Fyn and prevents both Asso-induced Fyn signaling and downstream phosphorylation of the AD risk gene product Pyk2, and of NR2B Glu receptors in brain slices. saracatinib 9-16 Fyn proto-oncogene Mus musculus 35-38 25707991-9 2015 RESULTS: AZD0530 potently inhibits Fyn and prevents both Asso-induced Fyn signaling and downstream phosphorylation of the AD risk gene product Pyk2, and of NR2B Glu receptors in brain slices. saracatinib 9-16 Fyn proto-oncogene Mus musculus 70-73 25707991-9 2015 RESULTS: AZD0530 potently inhibits Fyn and prevents both Asso-induced Fyn signaling and downstream phosphorylation of the AD risk gene product Pyk2, and of NR2B Glu receptors in brain slices. saracatinib 9-16 PTK2 protein tyrosine kinase 2 beta Mus musculus 143-147 25707991-9 2015 RESULTS: AZD0530 potently inhibits Fyn and prevents both Asso-induced Fyn signaling and downstream phosphorylation of the AD risk gene product Pyk2, and of NR2B Glu receptors in brain slices. saracatinib 9-16 glutamate receptor, ionotropic, NMDA2B (epsilon 2) Mus musculus 156-160 25707991-10 2015 After 4 weeks of treatment, AZD0530 dosing of APP/PS1 transgenic mice fully rescues spatial memory deficits and synaptic depletion, without altering APP or Ass metabolism. saracatinib 28-35 presenilin 1 Mus musculus 50-53 25707991-11 2015 AZD0530 treatment also reduces microglial activation in APP/PS1 mice, and rescues Tau phosphorylation and deposition abnormalities in APP/PS1/Tau transgenic mice. saracatinib 0-7 presenilin 1 Mus musculus 60-63 25707991-11 2015 AZD0530 treatment also reduces microglial activation in APP/PS1 mice, and rescues Tau phosphorylation and deposition abnormalities in APP/PS1/Tau transgenic mice. saracatinib 0-7 presenilin 1 Mus musculus 138-141 25874001-5 2015 Herein, we present a Phase Ib trial of the repurposed investigational drug AZD0530, a Src family kinase inhibitor specific for Fyn and Src kinase, for the treatment of patients with mild-to-moderate AD. saracatinib 75-82 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 127-130 25662515-12 2015 The Src and BCR-Abl inhibitors saracatinib and AZD0424, along with the previous four drugs, are in clinical trials for a variety of solid tumors including breast and lung cancers. saracatinib 31-42 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 4-7 25662515-12 2015 The Src and BCR-Abl inhibitors saracatinib and AZD0424, along with the previous four drugs, are in clinical trials for a variety of solid tumors including breast and lung cancers. saracatinib 31-42 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 12-19 25070546-1 2014 BACKGROUND: We investigated whether the Src inhibitor saracatinib (AZD0530) improved efficacy of weekly paclitaxel in platinum-resistant ovarian cancer. saracatinib 54-65 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 40-43 25338626-9 2015 The combination of bortezomib and saracatinib, a Src inhibitor, synergistically induced hepatoma cell apoptosis. saracatinib 34-45 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 25070546-1 2014 BACKGROUND: We investigated whether the Src inhibitor saracatinib (AZD0530) improved efficacy of weekly paclitaxel in platinum-resistant ovarian cancer. saracatinib 67-74 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 40-43 25226534-8 2014 Moreover, combination of SP600125 and the Src inhibitor saracatinib synergistically inhibits cell proliferation. saracatinib 56-67 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 42-45 25047515-4 2014 The Src kinase inhibitor AZD0530 (saracatinib) blocked TGF-beta1-induced Src kinase activation in a dose-dependent manner. saracatinib 25-32 transforming growth factor, beta 1 Mus musculus 55-64 25047515-4 2014 The Src kinase inhibitor AZD0530 (saracatinib) blocked TGF-beta1-induced Src kinase activation in a dose-dependent manner. saracatinib 34-45 transforming growth factor, beta 1 Mus musculus 55-64 25047515-6 2014 In addition, the induced expression of collagen and fibronectin and three-dimensional collagen gel contraction were also significantly inhibited in AZD0530-treated fibroblasts. saracatinib 148-155 fibronectin 1 Mus musculus 52-63 25047515-9 2014 Furthermore, the total fibrotic area and expression of alpha-SMA and ECM proteins were significantly decreased in lungs of AZD0530-treated mice. saracatinib 123-130 actin alpha 2, smooth muscle, aorta Mus musculus 55-64 25108485-6 2014 JAR and JEG-3 cells were treated with hCG, specific c-Src inhibitor saracatinib and PP2, and PKA specific inhibitor, PKI. saracatinib 68-79 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 52-57 25108485-10 2014 Inhibition of c-Src activity in JAR and JEG-3 cells by saracatinib leaded to a decrease in the rate of cell growth and cell migration/invasion ability. saracatinib 55-66 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-19 24828915-3 2014 Here, we report the development of a small molecule probe of Src through conjugation of BODIPY to two well-established dual Src-Abl kinase inhibitors, dasatinib and saracatinib. saracatinib 165-176 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 61-64 25114223-5 2014 This approach identified a number of kinase inhibitors that robustly up-regulate IL-10 production including the Food and Drug Administration (FDA)-approved drugs dasatinib, bosutinib, and saracatinib that target ABL, SRC-family, and numerous other kinases. saracatinib 188-199 interleukin 10 Homo sapiens 81-86 25114223-5 2014 This approach identified a number of kinase inhibitors that robustly up-regulate IL-10 production including the Food and Drug Administration (FDA)-approved drugs dasatinib, bosutinib, and saracatinib that target ABL, SRC-family, and numerous other kinases. saracatinib 188-199 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 212-215 25114223-5 2014 This approach identified a number of kinase inhibitors that robustly up-regulate IL-10 production including the Food and Drug Administration (FDA)-approved drugs dasatinib, bosutinib, and saracatinib that target ABL, SRC-family, and numerous other kinases. saracatinib 188-199 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 217-220 24968896-3 2014 Since Src is frequently activated in ovarian cancers, we investigated whether combined Src and ER blockade by saracatinib and fulvestrant would circumvent anti-estrogen resistance. saracatinib 110-121 estrogen receptor 1 Homo sapiens 95-97 24968896-9 2014 Combined saracatinib and fulvestrant increased p27 and inhibited cell cycle progression. saracatinib 9-20 interferon alpha inducible protein 27 Homo sapiens 47-50 24968896-11 2014 Saracatinib facilitated the therapeutic effects of fulvestrant by antagonizing the estrogen-mediated Src activation. saracatinib 0-11 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 101-104 24713129-9 2014 However, lestaurtinib and saracatinib were identified as mechanism-based inhibitors of CYP3A. saracatinib 26-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-92 24713129-11 2014 Inhibition of CYP2C8 by bosutinib was predicted to have no clinical relevance, whereas therapeutic lestaurtinib and saracatinib concentrations were predicted to increase the plasma exposure to CYP3A-dependent substrates by >=2.7-fold. saracatinib 116-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 193-198 24828915-3 2014 Here, we report the development of a small molecule probe of Src through conjugation of BODIPY to two well-established dual Src-Abl kinase inhibitors, dasatinib and saracatinib. saracatinib 165-176 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 124-127 24492292-0 2014 The ErbB2-targeting antibody trastuzumab and the small-molecule SRC inhibitor saracatinib synergistically inhibit ErbB2-overexpressing gastric cancer. saracatinib 78-89 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 64-67 24612061-7 2014 A Src inhibitor saracatinib impaired growth in cell lines that are insensitive to both Met and FGFR2 inhibitors. saracatinib 16-27 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 2-5 24612061-8 2014 Saracatinib also effectively impaired peritoneal dissemination of Met-independent and FGFR2-independent SGC cells. saracatinib 0-11 fibroblast growth factor receptor 2 Homo sapiens 86-91 24887236-8 2014 The selective small-molecule Src inhibitor saracatinib combined with lapatinib synergistically inhibited the proliferation, migration, and invasion of lapatinib-resistant cells. saracatinib 43-54 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 29-32 24361364-13 2014 AZD0530 treatment demonstrated restoration of Cx43 comparable to PP1. saracatinib 0-7 gap junction protein, alpha 1 Mus musculus 46-50 24111605-9 2014 AZD-0530 treatment blocked c-Src activation, decreased macrophage influx, and prevented airspace enlargement in the lungs of cigarette smoke-exposed mice. saracatinib 0-8 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 27-32 24492292-0 2014 The ErbB2-targeting antibody trastuzumab and the small-molecule SRC inhibitor saracatinib synergistically inhibit ErbB2-overexpressing gastric cancer. saracatinib 78-89 erb-b2 receptor tyrosine kinase 2 Homo sapiens 114-119 24492292-2 2014 Here, we investigated the antitumor activity of the combination of trastuzumab and the SRC inhibitor saracatinib in ErbB2-overexpressing trastuzumab-resistant gastric cancer. saracatinib 101-112 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 87-90 24492292-2 2014 Here, we investigated the antitumor activity of the combination of trastuzumab and the SRC inhibitor saracatinib in ErbB2-overexpressing trastuzumab-resistant gastric cancer. saracatinib 101-112 erb-b2 receptor tyrosine kinase 2 Homo sapiens 116-121 24492292-5 2014 Our data demonstrated that trastuzumab plus saracatinib was much more potent than either agent alone in reducing the phosphorylation of ErbB3 and AKT in both NCI-N87 and NCI-N87R gastric cancer cell lines. saracatinib 44-55 erb-b2 receptor tyrosine kinase 3 Homo sapiens 136-141 24492292-5 2014 Our data demonstrated that trastuzumab plus saracatinib was much more potent than either agent alone in reducing the phosphorylation of ErbB3 and AKT in both NCI-N87 and NCI-N87R gastric cancer cell lines. saracatinib 44-55 AKT serine/threonine kinase 1 Homo sapiens 146-149 24492292-7 2014 Further data showed that combination therapy of trastuzumab with saracatinib resulted in a significant benefit over either agent alone in both NCI-N87 and NCI-N87R xenograft models, suggesting its potential use for treating ErbB2-overexpressing gastric cancer. saracatinib 65-76 erb-b2 receptor tyrosine kinase 2 Homo sapiens 224-229 24169259-0 2014 A phase II trial of saracatinib, an inhibitor of src kinases, in previously-treated advanced non-small-cell lung cancer: the princess margaret hospital phase II consortium. saracatinib 20-31 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 24495408-5 2014 We are currently enrolling patients in a phase Ib study of saracatinib (AZD0530), a small molecule inhibitor with high potency for Src and Fyn, for the treatment of AD. saracatinib 59-70 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 131-134 24495408-5 2014 We are currently enrolling patients in a phase Ib study of saracatinib (AZD0530), a small molecule inhibitor with high potency for Src and Fyn, for the treatment of AD. saracatinib 59-70 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 139-142 24495408-5 2014 We are currently enrolling patients in a phase Ib study of saracatinib (AZD0530), a small molecule inhibitor with high potency for Src and Fyn, for the treatment of AD. saracatinib 72-79 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 131-134 24495408-5 2014 We are currently enrolling patients in a phase Ib study of saracatinib (AZD0530), a small molecule inhibitor with high potency for Src and Fyn, for the treatment of AD. saracatinib 72-79 FYN proto-oncogene, Src family tyrosine kinase Homo sapiens 139-142 24200972-6 2014 Treatment with the Src inhibitor saracatinib in combination with lapatinib reduces AKT and ERK1/2 phosphorylation and restores the sensitivity of resistant cells to lapatinib. saracatinib 33-44 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 19-22 24200972-6 2014 Treatment with the Src inhibitor saracatinib in combination with lapatinib reduces AKT and ERK1/2 phosphorylation and restores the sensitivity of resistant cells to lapatinib. saracatinib 33-44 AKT serine/threonine kinase 1 Homo sapiens 83-86 24200972-6 2014 Treatment with the Src inhibitor saracatinib in combination with lapatinib reduces AKT and ERK1/2 phosphorylation and restores the sensitivity of resistant cells to lapatinib. saracatinib 33-44 mitogen-activated protein kinase 3 Homo sapiens 91-97 24169259-2 2014 The activity of saracatinib, an orally available inhibitor of src kinases, was evaluated in patients with advanced, platinum-pretreated NSCLC. saracatinib 16-27 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 62-65 23948603-11 2013 Given reports that SRC inhibitors can block Id1 expression, we tested the SRC inhibitor, AZD0530, and found that it inhibits the serum activation of Id1. saracatinib 89-96 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 19-22 24201814-0 2013 An EMT spectrum defines an anoikis-resistant and spheroidogenic intermediate mesenchymal state that is sensitive to e-cadherin restoration by a src-kinase inhibitor, saracatinib (AZD0530). saracatinib 166-177 cadherin 1 Homo sapiens 116-126 24201814-0 2013 An EMT spectrum defines an anoikis-resistant and spheroidogenic intermediate mesenchymal state that is sensitive to e-cadherin restoration by a src-kinase inhibitor, saracatinib (AZD0530). saracatinib 179-186 cadherin 1 Homo sapiens 116-126 24201814-7 2013 A specific Src-kinase inhibitor, Saracatinib (AZD0530), restores E-cadherin expression in Intermediate M cells in in vitro and in vivo models and abrogates spheroidogenesis. saracatinib 33-44 cadherin 1 Homo sapiens 65-75 24201814-7 2013 A specific Src-kinase inhibitor, Saracatinib (AZD0530), restores E-cadherin expression in Intermediate M cells in in vitro and in vivo models and abrogates spheroidogenesis. saracatinib 46-53 cadherin 1 Homo sapiens 65-75 23948603-13 2013 Rather, we show that AZD0530 directly inhibits the BMP type I receptors. saracatinib 21-28 bone morphogenetic protein 1 Homo sapiens 51-54 23948603-11 2013 Given reports that SRC inhibitors can block Id1 expression, we tested the SRC inhibitor, AZD0530, and found that it inhibits the serum activation of Id1. saracatinib 89-96 inhibitor of DNA binding 1, HLH protein Homo sapiens 44-47 23948603-11 2013 Given reports that SRC inhibitors can block Id1 expression, we tested the SRC inhibitor, AZD0530, and found that it inhibits the serum activation of Id1. saracatinib 89-96 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 74-77 23948603-11 2013 Given reports that SRC inhibitors can block Id1 expression, we tested the SRC inhibitor, AZD0530, and found that it inhibits the serum activation of Id1. saracatinib 89-96 inhibitor of DNA binding 1, HLH protein Homo sapiens 149-152 22415795-0 2013 First report of the safety, tolerability, and pharmacokinetics of the Src kinase inhibitor saracatinib (AZD0530) in Japanese patients with advanced solid tumours. saracatinib 91-102 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 70-73 22415795-0 2013 First report of the safety, tolerability, and pharmacokinetics of the Src kinase inhibitor saracatinib (AZD0530) in Japanese patients with advanced solid tumours. saracatinib 104-111 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 70-73 22415795-1 2013 BACKGROUND: Saracatinib (AZD0530) is a selective, oral Src inhibitor that has demonstrated antitumour activity in preclinical studies. saracatinib 12-23 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 55-58 22415795-1 2013 BACKGROUND: Saracatinib (AZD0530) is a selective, oral Src inhibitor that has demonstrated antitumour activity in preclinical studies. saracatinib 25-32 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 55-58 22623106-0 2013 Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo. saracatinib 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 22310287-9 2013 This mode of invasion is dependent on integrin-mediated adhesion, and because SRC kinases are the main regulators of this process, the SRC kinase inhibitor, saracatinib (AZD0530), completely abolished the MEK inhibitor-induced invasion. saracatinib 157-168 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 78-81 22310287-9 2013 This mode of invasion is dependent on integrin-mediated adhesion, and because SRC kinases are the main regulators of this process, the SRC kinase inhibitor, saracatinib (AZD0530), completely abolished the MEK inhibitor-induced invasion. saracatinib 157-168 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 135-138 22310287-9 2013 This mode of invasion is dependent on integrin-mediated adhesion, and because SRC kinases are the main regulators of this process, the SRC kinase inhibitor, saracatinib (AZD0530), completely abolished the MEK inhibitor-induced invasion. saracatinib 157-168 mitogen-activated protein kinase kinase 7 Homo sapiens 205-208 22310287-9 2013 This mode of invasion is dependent on integrin-mediated adhesion, and because SRC kinases are the main regulators of this process, the SRC kinase inhibitor, saracatinib (AZD0530), completely abolished the MEK inhibitor-induced invasion. saracatinib 170-177 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 78-81 22310287-9 2013 This mode of invasion is dependent on integrin-mediated adhesion, and because SRC kinases are the main regulators of this process, the SRC kinase inhibitor, saracatinib (AZD0530), completely abolished the MEK inhibitor-induced invasion. saracatinib 170-177 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 135-138 22310287-9 2013 This mode of invasion is dependent on integrin-mediated adhesion, and because SRC kinases are the main regulators of this process, the SRC kinase inhibitor, saracatinib (AZD0530), completely abolished the MEK inhibitor-induced invasion. saracatinib 170-177 mitogen-activated protein kinase kinase 7 Homo sapiens 205-208 22310287-10 2013 Moreover, the combination of saracatinib and selumetinib effectively suppressed the growth and invasion of melanoma cells in a 3D environment, suggesting that combined inhibition of MEK and SRC is a promising approach to improve the efficacy of targeting the ERK/MAP kinase pathway in melanoma. saracatinib 29-40 mitogen-activated protein kinase kinase 7 Homo sapiens 182-185 22310287-10 2013 Moreover, the combination of saracatinib and selumetinib effectively suppressed the growth and invasion of melanoma cells in a 3D environment, suggesting that combined inhibition of MEK and SRC is a promising approach to improve the efficacy of targeting the ERK/MAP kinase pathway in melanoma. saracatinib 29-40 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 190-193 22310287-10 2013 Moreover, the combination of saracatinib and selumetinib effectively suppressed the growth and invasion of melanoma cells in a 3D environment, suggesting that combined inhibition of MEK and SRC is a promising approach to improve the efficacy of targeting the ERK/MAP kinase pathway in melanoma. saracatinib 29-40 mitogen-activated protein kinase 1 Homo sapiens 259-262 22623106-0 2013 Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo. saracatinib 13-20 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 22623106-1 2013 Saracatinib, a highly selective, dual Src/Abl kinase inhibitor, is currently in a Phase II clinical trial for the treatment of ovarian cancer. saracatinib 0-11 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 38-41 22623106-3 2013 Our results showed that saracatinib significantly enhanced the cytotoxicity of ABCB1 substrate drugs in ABCB1 overexpressing HeLa/v200, MCF-7/adr and HEK293/ABCB1 cells, an effect that was stronger than that of gefitinib, whereas it had no effect on the cytotoxicity of the substrates in ABCC1 overexpressing HL-60/adr cells and its parental sensitive cells. saracatinib 24-35 ATP binding cassette subfamily B member 1 Homo sapiens 79-84 22623106-3 2013 Our results showed that saracatinib significantly enhanced the cytotoxicity of ABCB1 substrate drugs in ABCB1 overexpressing HeLa/v200, MCF-7/adr and HEK293/ABCB1 cells, an effect that was stronger than that of gefitinib, whereas it had no effect on the cytotoxicity of the substrates in ABCC1 overexpressing HL-60/adr cells and its parental sensitive cells. saracatinib 24-35 ATP binding cassette subfamily B member 1 Homo sapiens 104-109 22623106-3 2013 Our results showed that saracatinib significantly enhanced the cytotoxicity of ABCB1 substrate drugs in ABCB1 overexpressing HeLa/v200, MCF-7/adr and HEK293/ABCB1 cells, an effect that was stronger than that of gefitinib, whereas it had no effect on the cytotoxicity of the substrates in ABCC1 overexpressing HL-60/adr cells and its parental sensitive cells. saracatinib 24-35 ATP binding cassette subfamily B member 1 Homo sapiens 104-109 22623106-3 2013 Our results showed that saracatinib significantly enhanced the cytotoxicity of ABCB1 substrate drugs in ABCB1 overexpressing HeLa/v200, MCF-7/adr and HEK293/ABCB1 cells, an effect that was stronger than that of gefitinib, whereas it had no effect on the cytotoxicity of the substrates in ABCC1 overexpressing HL-60/adr cells and its parental sensitive cells. saracatinib 24-35 ATP binding cassette subfamily C member 1 Homo sapiens 288-293 22623106-5 2013 Furthermore, saracatinib stimulated the ATPase activity and inhibited photolabeling of ABCB1 with [(125)I]-iodoarylazidoprazosin in a concentration-dependent manner. saracatinib 13-24 ATP binding cassette subfamily B member 1 Homo sapiens 87-92 22623106-6 2013 In addition, the homology modeling predicted the binding conformation of saracatinib within the large hydrophobic drug-binding cavity of human ABCB1. saracatinib 73-84 ATP binding cassette subfamily B member 1 Homo sapiens 143-148 22623106-8 2013 Importantly, saracatinib significantly enhanced the effect of paclitaxel against ABCB1-overexpressing HeLa/v200 cancer cell xenografts in nude mice. saracatinib 13-24 ATP binding cassette subfamily B member 1 Homo sapiens 81-86 22623106-9 2013 In conclusion, saracatinib reverses ABCB1-mediated MDR in vitro and in vivo by directly inhibiting ABCB1 transport function, without altering ABCB1 expression or AKT phosphorylation. saracatinib 15-26 ATP binding cassette subfamily B member 1 Homo sapiens 36-41 22623106-9 2013 In conclusion, saracatinib reverses ABCB1-mediated MDR in vitro and in vivo by directly inhibiting ABCB1 transport function, without altering ABCB1 expression or AKT phosphorylation. saracatinib 15-26 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 22623106-9 2013 In conclusion, saracatinib reverses ABCB1-mediated MDR in vitro and in vivo by directly inhibiting ABCB1 transport function, without altering ABCB1 expression or AKT phosphorylation. saracatinib 15-26 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 23144237-0 2013 Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer. saracatinib 22-33 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 47-52 23144237-0 2013 Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer. saracatinib 35-42 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 47-52 23144237-4 2013 We evaluated the antitumor effect of a c-Src/Abl kinase inhibitor, saracatinib (AZD0530), alone or combined with chemotherapeutic agents in gastric cancer cell lines and a NCI-N87 xenograft model. saracatinib 67-78 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 39-44 23144237-6 2013 Saracatinib blocked the Src/FAK, HER family, and oncogenic signaling pathways, and it induced G(1) arrest and apoptosis in SNU216 and NCI-N87 cells. saracatinib 0-11 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 24-27 23144237-6 2013 Saracatinib blocked the Src/FAK, HER family, and oncogenic signaling pathways, and it induced G(1) arrest and apoptosis in SNU216 and NCI-N87 cells. saracatinib 0-11 protein tyrosine kinase 2 Homo sapiens 28-31 23144237-8 2013 Knockdown of Bim using siRNA decreased apoptosis induced by treatment with saracatinib, suggesting that Bim has an important role in saracatinib-induced apoptosis. saracatinib 75-86 BCL2 like 11 Homo sapiens 13-16 23144237-8 2013 Knockdown of Bim using siRNA decreased apoptosis induced by treatment with saracatinib, suggesting that Bim has an important role in saracatinib-induced apoptosis. saracatinib 75-86 BCL2 like 11 Homo sapiens 104-107 23144237-8 2013 Knockdown of Bim using siRNA decreased apoptosis induced by treatment with saracatinib, suggesting that Bim has an important role in saracatinib-induced apoptosis. saracatinib 133-144 BCL2 like 11 Homo sapiens 13-16 23144237-8 2013 Knockdown of Bim using siRNA decreased apoptosis induced by treatment with saracatinib, suggesting that Bim has an important role in saracatinib-induced apoptosis. saracatinib 133-144 BCL2 like 11 Homo sapiens 104-107 23144237-9 2013 Saracatinib enhanced the effects of lapatinib, an EGFR/HER2 dual inhibitor, in SNU216 and NCI-N87 cells. saracatinib 0-11 epidermal growth factor receptor Homo sapiens 50-54 23144237-9 2013 Saracatinib enhanced the effects of lapatinib, an EGFR/HER2 dual inhibitor, in SNU216 and NCI-N87 cells. saracatinib 0-11 erb-b2 receptor tyrosine kinase 2 Homo sapiens 55-59 23144237-12 2013 These data indicate that the inhibition of Src kinase activity by saracatinib alone or in combination with other agents can be a strategy to target gastric cancer. saracatinib 66-77 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 43-46 23342270-0 2012 Biomarker-driven trial in metastatic pancreas cancer: feasibility in a multicenter study of saracatinib, an oral Src inhibitor, in previously treated pancreatic cancer. saracatinib 92-103 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 113-116 22896656-0 2012 Src Inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo. saracatinib 20-31 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 0-3 22896656-0 2012 Src Inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo. saracatinib 20-31 estrogen receptor 1 Homo sapiens 67-69 22896656-4 2012 Because Src is activated in most ovarian cancers, we investigated whether combined Src and ER blockade by saracatinib and fulvestrant would circumvent antiestrogen resistance. saracatinib 106-117 estrogen receptor 1 Homo sapiens 91-93 22896656-11 2012 While each alone had little effect, combined saracatinib and fulvestrant increased p27 and inhibited cyclin E-Cdk2 and cell-cycle progression. saracatinib 45-56 interferon alpha inducible protein 27 Homo sapiens 83-86 22896656-12 2012 Saracatinib also impaired induction of ER-target genes c-Myc and FOSL1; this was greatest with dual therapy. saracatinib 0-11 MYC proto-oncogene, bHLH transcription factor Homo sapiens 55-60 22896656-12 2012 Saracatinib also impaired induction of ER-target genes c-Myc and FOSL1; this was greatest with dual therapy. saracatinib 0-11 FOS like 1, AP-1 transcription factor subunit Homo sapiens 65-70 22896656-14 2012 CONCLUSIONS: Saracatinib augments effects of fulvestrant by opposing estrogen-mediated Src activation and target gene expression, increasing cell-cycle arrest, and impairing survival, all of which would oppose antiestrogen resistance in these ER+ ovarian cancer models. saracatinib 13-24 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 87-90 23342270-1 2012 Src tyrosine kinases are overexpressed in pancreatic cancers, and the oral Src inhibitor saracatinib has shown antitumor activity in preclinical models of pancreas cancer. saracatinib 89-100 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 75-78 21989836-0 2012 Phase I open-label study of cediranib, an oral inhibitor of VEGF signalling, in combination with the oral Src inhibitor saracatinib in patients with advanced solid tumours. saracatinib 120-131 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 106-109 22526632-5 2012 In the present studies, we have examined the ability of saracatinib, a dual-specific, orally available inhibitor of Src and Abl protein tyrosine kinases, to interfere with the establishment of lung metastases in mice by tumor cells introduced into the blood stream. saracatinib 56-67 Rous sarcoma oncogene Mus musculus 116-119 22249264-4 2012 Incubation of lung cancer cells with the Src inhibitor saracatinib led to the upregulation of several miRNAs including miR-29b, which was the most highly upregulated miRNA with predicted binding to the ID1 3"-untranslated region (UTR). saracatinib 55-66 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 41-44 22249264-4 2012 Incubation of lung cancer cells with the Src inhibitor saracatinib led to the upregulation of several miRNAs including miR-29b, which was the most highly upregulated miRNA with predicted binding to the ID1 3"-untranslated region (UTR). saracatinib 55-66 microRNA 29b-1 Homo sapiens 119-126 22249264-4 2012 Incubation of lung cancer cells with the Src inhibitor saracatinib led to the upregulation of several miRNAs including miR-29b, which was the most highly upregulated miRNA with predicted binding to the ID1 3"-untranslated region (UTR). saracatinib 55-66 inhibitor of DNA binding 1, HLH protein Homo sapiens 202-205 22249264-9 2012 Both, anti-miR-29b and ID1 overexpression diminished the effects of the Src inhibitors saracatinib and dasatinib on migration and invasion. saracatinib 87-98 microRNA 29b-1 Homo sapiens 11-18 22249264-9 2012 Both, anti-miR-29b and ID1 overexpression diminished the effects of the Src inhibitors saracatinib and dasatinib on migration and invasion. saracatinib 87-98 inhibitor of DNA binding 1, HLH protein Homo sapiens 23-26 22249264-9 2012 Both, anti-miR-29b and ID1 overexpression diminished the effects of the Src inhibitors saracatinib and dasatinib on migration and invasion. saracatinib 87-98 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 72-75 22249264-10 2012 Saracatinib and dasatinib decreased c-Myc transcriptional repression on miR-29b and led to increased ID1 protein levels, whereas forced expression of c-Myc repressed miR-29b and induced ID1. saracatinib 0-11 microRNA 29b-1 Homo sapiens 72-79 22249264-10 2012 Saracatinib and dasatinib decreased c-Myc transcriptional repression on miR-29b and led to increased ID1 protein levels, whereas forced expression of c-Myc repressed miR-29b and induced ID1. saracatinib 0-11 inhibitor of DNA binding 1, HLH protein Homo sapiens 101-104 22526632-5 2012 In the present studies, we have examined the ability of saracatinib, a dual-specific, orally available inhibitor of Src and Abl protein tyrosine kinases, to interfere with the establishment of lung metastases in mice by tumor cells introduced into the blood stream. saracatinib 56-67 c-abl oncogene 1, non-receptor tyrosine kinase Mus musculus 124-127 22452946-0 2012 Antitumor activity of Src inhibitor saracatinib (AZD-0530) in preclinical models of biliary tract carcinomas. saracatinib 36-47 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 22-25 22452946-0 2012 Antitumor activity of Src inhibitor saracatinib (AZD-0530) in preclinical models of biliary tract carcinomas. saracatinib 49-57 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 22-25 22452946-3 2012 Among potential candidate molecules, we evaluated the nonreceptor tyrosine kinase Src, observing promising antitumor effects of its small-molecule inhibitor saracatinib in BTC preclinical models. saracatinib 157-168 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 82-85 22452946-5 2012 Upon saracatinib treatment, the phosphorylation of Src and of its downstream transducers was evaluated in the BTC cell lines TFK-1, EGI-1, HuH28, and TGBC1-TKB. saracatinib 5-16 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 51-54 22452946-9 2012 In cultured BTC cell lines, low-dose saracatinib counteracted the activation of Src and of its downstream effectors, increased the fraction of cells in G(0)-G(1) phase, and inhibited cell migration. saracatinib 37-48 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 80-83 22452946-12 2012 Here, we provide a demonstration that the targeted inhibition of Src kinase by saracatinib is of therapeutic benefit in preclinical models of BTC. saracatinib 79-90 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 65-68 21894461-5 2012 Inhibition of Src kinase activity using the inhibitors PP2 or saracatinib or using siRNA abrogates the preferential migration of the breast cancer cell lines in response to bone-derived cells. saracatinib 62-73 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 21792888-5 2012 Activation of migration related components FAK, P130Cas and Paxillin were blocked by saracatinib at 0.05- to 3-muM concentrations. saracatinib 85-96 BCAR1 scaffold protein, Cas family member Homo sapiens 48-55 21792888-7 2012 Molecular studies in Caki-1 showed that saracatinib alone and in combination with sunitinib inhibited phosphorylation of the cell progression regulator c-Myc in a dose-dependent manner. saracatinib 40-51 MYC proto-oncogene, bHLH transcription factor Homo sapiens 152-157 21792888-10 2012 HIF1-alpha expression in normoxic and hypoxic conditions in Caki-1 cells was inhibited by either saracatinib or sunitinib when administered alone, however, a greater reduction occurred when these compounds were given in combination. saracatinib 97-108 hypoxia inducible factor 1 subunit alpha Homo sapiens 0-10 22592211-7 2012 The Src tyrosine kinase inhibitors saracatinib and dasatinib were used to repress ID1 expression. saracatinib 35-46 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 4-7 22592211-7 2012 The Src tyrosine kinase inhibitors saracatinib and dasatinib were used to repress ID1 expression. saracatinib 35-46 inhibitor of DNA binding 1, HLH protein Homo sapiens 82-85 22596237-3 2012 METHODS: First, in investigating imaging biomarkers of invasion, the response of orthotopic murine PC3 prostate xenografts to the Src inhibitor saracatinib was assessed using susceptibility contrast MRI. saracatinib 144-155 chromobox 8 Mus musculus 99-102 22596237-3 2012 METHODS: First, in investigating imaging biomarkers of invasion, the response of orthotopic murine PC3 prostate xenografts to the Src inhibitor saracatinib was assessed using susceptibility contrast MRI. saracatinib 144-155 Rous sarcoma oncogene Mus musculus 130-133 22596237-5 2012 RESULTS: No significant differences in fractional blood volume (%), vessel calibre (mum), native T(1) (ms) or apparent water diffusion coefficient were determined, despite reduced expression of activated Fak and paxillin in the saracatinib cohort. saracatinib 228-239 paxillin Rattus norvegicus 212-220 21400081-0 2012 A phase II trial of the Src kinase inhibitor saracatinib (AZD0530) in patients with metastatic or locally advanced gastric or gastro esophageal junction (GEJ) adenocarcinoma: a trial of the PMH phase II consortium. saracatinib 45-56 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 24-27 21400081-0 2012 A phase II trial of the Src kinase inhibitor saracatinib (AZD0530) in patients with metastatic or locally advanced gastric or gastro esophageal junction (GEJ) adenocarcinoma: a trial of the PMH phase II consortium. saracatinib 58-65 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 24-27 21400081-2 2012 We evaluated the activity and safety of saracatinib an oral, anilinoquinazolone, non-receptor tyrosine kinase inhibitor targeting Src kinases, in patients with metastatic or locally advanced gastric carcinoma. saracatinib 40-51 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 130-133 21894461-6 2012 Inhibition of Src activity with saracatinib does not have any significant effect on breast cancer cell invasion in the presence of bone-derived cells. saracatinib 32-43 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 22553375-0 2012 Common PIK3CA mutants and a novel 3" UTR mutation are associated with increased sensitivity to saracatinib. saracatinib 95-106 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 7-13 22553375-6 2012 Mutations in the PIK3CA were evaluated to examine the association between mutations in the PIK3CA gene and sensitivity to saracatinib. saracatinib 122-133 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 91-97 22553375-7 2012 RESULTS: We have identified a subset of patients with a PIK3CA (exon 9 and 20) mutation with increased sensitivity to saracatinib. saracatinib 118-129 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 56-62 22450814-5 2012 Saracatinib, a specific inhibitor of Src family kinases, administered at low doses during the expansion or contraction phases, increased CD62L(high)/CD44(high) central memory CD8(+) T cells and IFN-gamma production but suppressed immunity when added during the priming phase. saracatinib 0-11 selectin, lymphocyte Mus musculus 137-142 22450814-5 2012 Saracatinib, a specific inhibitor of Src family kinases, administered at low doses during the expansion or contraction phases, increased CD62L(high)/CD44(high) central memory CD8(+) T cells and IFN-gamma production but suppressed immunity when added during the priming phase. saracatinib 0-11 CD44 antigen Mus musculus 149-153 22450814-5 2012 Saracatinib, a specific inhibitor of Src family kinases, administered at low doses during the expansion or contraction phases, increased CD62L(high)/CD44(high) central memory CD8(+) T cells and IFN-gamma production but suppressed immunity when added during the priming phase. saracatinib 0-11 interferon gamma Mus musculus 194-203 22450814-6 2012 These effects by saracatinib were not accompanied by the expected decline of Src family kinases but were accompanied by Akt-mammalian target of rapamycin suppression and/or mediated via another pathway. saracatinib 17-28 AKT serine/threonine kinase 1 Homo sapiens 120-123 22450814-6 2012 These effects by saracatinib were not accompanied by the expected decline of Src family kinases but were accompanied by Akt-mammalian target of rapamycin suppression and/or mediated via another pathway. saracatinib 17-28 mechanistic target of rapamycin kinase Homo sapiens 124-153 22326918-8 2012 In addition, we found that treatment with AZD-0530, a pharmacological Src inhibitor, reduced the regulatory effect of TRAF6 knockdown on VEGF promoter activity. saracatinib 42-50 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 70-73 21170669-0 2012 A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer. saracatinib 40-51 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 26-29 21170669-0 2012 A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer. saracatinib 53-60 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 26-29 22326918-8 2012 In addition, we found that treatment with AZD-0530, a pharmacological Src inhibitor, reduced the regulatory effect of TRAF6 knockdown on VEGF promoter activity. saracatinib 42-50 TNF receptor associated factor 6 Homo sapiens 118-123 22326918-8 2012 In addition, we found that treatment with AZD-0530, a pharmacological Src inhibitor, reduced the regulatory effect of TRAF6 knockdown on VEGF promoter activity. saracatinib 42-50 vascular endothelial growth factor A Homo sapiens 137-141 22471705-4 2012 There are currently four Src inhibitors (dasatinib, saracatinib, bosutinib, and KX01) in clinical development, and although there is a plethora of information on their activity in preclinical models their clinical efficacy has been disappointing. saracatinib 52-63 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 25-28 22157722-5 2012 AZD0530 is a Src TKI, TSA is a histone deacetylase inhibitor, and ABT-263 is a Bcl-2 inhibitor. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 13-16 22369552-6 2012 To confirm that TGF-beta3 plays a role in epithelial barrier function, a selective Src family kinase inhibitor saracatinib (AZD0530) was added to cells treated with active TGF-beta3. saracatinib 111-122 transforming growth factor beta 3 Homo sapiens 16-25 21863025-8 2011 In addition, CR-1 significantly increased the invasive ability of melanoma cells that was prevented by treatment with either the ALK4 inhibitor SB-431542 or the c-Src inhibitor saracatinib (AZD0530). saracatinib 177-188 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 161-166 21994334-8 2011 Importantly, LHBs-induced cellular proliferation and tumor formation were reversed by administration of the Src inhibitor saracatinib. saracatinib 122-133 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 108-111 21499296-8 2011 Finally, the combination of lapatinib and the Src inhibitor AZD0530 was more effective than lapatinib alone at inhibiting pAkt and growth of established HER2-positive BT-474 xenografts in athymic mice. saracatinib 60-67 Rous sarcoma oncogene Mus musculus 46-49 21499296-8 2011 Finally, the combination of lapatinib and the Src inhibitor AZD0530 was more effective than lapatinib alone at inhibiting pAkt and growth of established HER2-positive BT-474 xenografts in athymic mice. saracatinib 60-67 erb-b2 receptor tyrosine kinase 2 Mus musculus 153-157 21729667-0 2011 Phase II trial of saracatinib (AZD0530), an oral SRC-inhibitor for the treatment of patients with hormone receptor-negative metastatic breast cancer. saracatinib 18-29 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 21729667-0 2011 Phase II trial of saracatinib (AZD0530), an oral SRC-inhibitor for the treatment of patients with hormone receptor-negative metastatic breast cancer. saracatinib 31-38 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 21729667-2 2011 Saracatinib is an oral tyrosine kinase inhibitor (TKI) selective for SRC. saracatinib 0-11 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 69-72 21729667-3 2011 We performed this trial to evaluate the efficacy and safety of saracatinib monotherapy in patients with estrogen receptor (ER)(-) and progesterone receptor (PR)(-) metastatic breast cancer (MBC). saracatinib 63-74 progesterone receptor Homo sapiens 134-155 21863025-8 2011 In addition, CR-1 significantly increased the invasive ability of melanoma cells that was prevented by treatment with either the ALK4 inhibitor SB-431542 or the c-Src inhibitor saracatinib (AZD0530). saracatinib 190-197 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 161-166 20630825-2 2010 Several Src inhibitors, including dasatinib, saracatinib, bosutinib, and KX2-391, are currently being investigated in clinical trials. saracatinib 45-56 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 8-11 20551056-6 2010 Saracatinib resembles the pharmacophore of known organic cation transporter (OCT) inhibitors and reduced oxaliplatin efficacy maximally in cells overexpressing OCT2. saracatinib 0-11 solute carrier family 22 member 2 Homo sapiens 160-164 20551056-7 2010 These data suggest that oxaliplatin uptake in CRC is attenuated by saracatinib via inhibition of OCT2, a potential consideration for the clinical development of this SFK inhibitor. saracatinib 67-78 solute carrier family 22 member 2 Homo sapiens 97-101 21642769-3 2011 In transformed cells, CHK1 inhibitor -induced activation of ERK1/2 was dependent upon activation of SRC family non-receptor tyrosine kinases as judged by use of multiple SRC kinase inhibitors (PP2, Dasatinib; AZD0530), use of SRC/FYN/YES deleted transformed fibroblasts or by expression of dominant negative SRC. saracatinib 209-216 checkpoint kinase 1 Homo sapiens 22-26 21642769-3 2011 In transformed cells, CHK1 inhibitor -induced activation of ERK1/2 was dependent upon activation of SRC family non-receptor tyrosine kinases as judged by use of multiple SRC kinase inhibitors (PP2, Dasatinib; AZD0530), use of SRC/FYN/YES deleted transformed fibroblasts or by expression of dominant negative SRC. saracatinib 209-216 mitogen-activated protein kinase 3 Homo sapiens 60-66 21642769-3 2011 In transformed cells, CHK1 inhibitor -induced activation of ERK1/2 was dependent upon activation of SRC family non-receptor tyrosine kinases as judged by use of multiple SRC kinase inhibitors (PP2, Dasatinib; AZD0530), use of SRC/FYN/YES deleted transformed fibroblasts or by expression of dominant negative SRC. saracatinib 209-216 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 100-103 20669046-3 2011 In this article, we show that treatment with the Src-inhibitor saracatinib (AZD0530) together with ER-blocking drugs increased breast cancer cell cycle arrest via p27. saracatinib 63-74 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 20669046-3 2011 In this article, we show that treatment with the Src-inhibitor saracatinib (AZD0530) together with ER-blocking drugs increased breast cancer cell cycle arrest via p27. saracatinib 63-74 estrogen receptor 1 Homo sapiens 99-101 20669046-3 2011 In this article, we show that treatment with the Src-inhibitor saracatinib (AZD0530) together with ER-blocking drugs increased breast cancer cell cycle arrest via p27. saracatinib 63-74 zinc ribbon domain containing 2 Homo sapiens 163-166 20669046-3 2011 In this article, we show that treatment with the Src-inhibitor saracatinib (AZD0530) together with ER-blocking drugs increased breast cancer cell cycle arrest via p27. saracatinib 76-83 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 20669046-3 2011 In this article, we show that treatment with the Src-inhibitor saracatinib (AZD0530) together with ER-blocking drugs increased breast cancer cell cycle arrest via p27. saracatinib 76-83 zinc ribbon domain containing 2 Homo sapiens 163-166 20669046-4 2011 Saracatinib and fulvestrant together more effectively increased p27, reduced Ki67, and impaired MDA-MB-361 xenograft tumor growth in vivo than either of the drugs alone. saracatinib 0-11 zinc ribbon domain containing 2 Homo sapiens 64-67 20669046-6 2011 Since combined ER and Src inhibition delays development of resistance in vivo, these data support further clinical investigation of saracatinib in combination with fulvestrant for women with ER-positive breast cancer. saracatinib 132-143 estrogen receptor 1 Homo sapiens 15-17 20669046-6 2011 Since combined ER and Src inhibition delays development of resistance in vivo, these data support further clinical investigation of saracatinib in combination with fulvestrant for women with ER-positive breast cancer. saracatinib 132-143 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 22-25 20669046-6 2011 Since combined ER and Src inhibition delays development of resistance in vivo, these data support further clinical investigation of saracatinib in combination with fulvestrant for women with ER-positive breast cancer. saracatinib 132-143 estrogen receptor 1 Homo sapiens 191-193 20669046-7 2011 Proteomic analysis revealed striking bypass activation of the mTOR pathway in saracatinib-resistant tumors. saracatinib 78-89 mechanistic target of rapamycin kinase Homo sapiens 62-66 20669046-8 2011 mTORC1 activation also arose following long-term culture of ER-positive breast cancer lines in the presence of saracatinib. saracatinib 111-122 CREB regulated transcription coactivator 1 Mus musculus 0-6 20669046-8 2011 mTORC1 activation also arose following long-term culture of ER-positive breast cancer lines in the presence of saracatinib. saracatinib 111-122 estrogen receptor 1 Homo sapiens 60-62 20669046-10 2011 The use of mTOR kinase inhibitors with saracatinib may subvert drug resistance and prove to be more effective than saracatinib alone. saracatinib 39-50 mechanistic target of rapamycin kinase Homo sapiens 11-15 20669046-10 2011 The use of mTOR kinase inhibitors with saracatinib may subvert drug resistance and prove to be more effective than saracatinib alone. saracatinib 115-126 mechanistic target of rapamycin kinase Homo sapiens 11-15 21461172-10 2011 An experimental Src kinase inhibitor, AZD0530, almost completely antagonized the TMZ-induced modulation in caveolin-1 expression. saracatinib 38-45 caveolin 1 Homo sapiens 107-117 21156787-7 2011 The treatment with Src inhibitors, such as PP2, dasatinib, and saracatinib, also suppressed the growth of A549 cells. saracatinib 63-74 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 19-22 21115886-2 2010 The aim of the present studies was to examine the impact of an Src inhibitor (saracatinib) on a highly metastatic murine sarcoma cell line (KHT). saracatinib 78-89 Rous sarcoma oncogene Mus musculus 63-66 21115886-6 2010 RESULTS: Saracatinib inhibited major pathways in the metastatic cascade in vitro, including Src and FAK activation. saracatinib 9-20 Rous sarcoma oncogene Mus musculus 92-95 21115886-6 2010 RESULTS: Saracatinib inhibited major pathways in the metastatic cascade in vitro, including Src and FAK activation. saracatinib 9-20 PTK2 protein tyrosine kinase 2 Mus musculus 100-103 21115886-9 2010 CONCLUSION: These findings suggest that Src inhibition by saracatinib may reduce the metastatic activity of tumor cells. saracatinib 58-69 Rous sarcoma oncogene Mus musculus 40-43 20805299-0 2010 Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors. saracatinib 74-85 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 52-55 20805299-1 2010 PURPOSE: This dose-escalation study evaluated the safety, tolerability, and pharmacokinetics (PK) of the oral Src inhibitor saracatinib (AZD0530) in patients with advanced solid malignancies. saracatinib 124-135 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 110-113 20805299-1 2010 PURPOSE: This dose-escalation study evaluated the safety, tolerability, and pharmacokinetics (PK) of the oral Src inhibitor saracatinib (AZD0530) in patients with advanced solid malignancies. saracatinib 137-144 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 110-113 20805299-2 2010 Tumor biopsy samples were taken to investigate the effect of saracatinib on Src activity in tumors. saracatinib 61-72 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 76-79 20805299-10 2010 Tumor Src activity was reduced following saracatinib treatment. saracatinib 41-52 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 6-9 20557276-6 2010 SKI-606 and AZD0530 are two other important dual Src/Abl inhibitors extensively tested in animal models and in clinical trials, but not entered into therapy yet. saracatinib 12-19 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 49-52 20557276-6 2010 SKI-606 and AZD0530 are two other important dual Src/Abl inhibitors extensively tested in animal models and in clinical trials, but not entered into therapy yet. saracatinib 12-19 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 53-56 20683035-1 2010 BACKGROUND: Saracatinib (AZD0530), a potent Src inhibitor, is a subject of current evaluation as an anticancer therapy. saracatinib 12-23 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 44-47 20683035-1 2010 BACKGROUND: Saracatinib (AZD0530), a potent Src inhibitor, is a subject of current evaluation as an anticancer therapy. saracatinib 25-32 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 44-47 20811583-5 2010 Previously, the authors reported that Src inhibitors such as saracatinib and PP2 caused G1 growth arrest and diminished invasiveness in prostate cancer cells but rarely apoptosis. saracatinib 61-72 Rous sarcoma oncogene Mus musculus 38-41 20484016-0 2010 Effect of the specific Src family kinase inhibitor saracatinib on osteolytic lesions using the PC-3 bone model. saracatinib 51-62 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 23-26 20484016-5 2010 We hypothesized that inhibiting Src activity with the specific Src family kinase inhibitor saracatinib (AZD0530) would inhibit tumor cell growth and osteoclast differentiation in the tumor-bone interface, thus providing a new approach for advanced prostate cancer. saracatinib 91-102 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 32-35 20484016-5 2010 We hypothesized that inhibiting Src activity with the specific Src family kinase inhibitor saracatinib (AZD0530) would inhibit tumor cell growth and osteoclast differentiation in the tumor-bone interface, thus providing a new approach for advanced prostate cancer. saracatinib 91-102 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 63-66 20484016-5 2010 We hypothesized that inhibiting Src activity with the specific Src family kinase inhibitor saracatinib (AZD0530) would inhibit tumor cell growth and osteoclast differentiation in the tumor-bone interface, thus providing a new approach for advanced prostate cancer. saracatinib 104-111 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 32-35 20484016-5 2010 We hypothesized that inhibiting Src activity with the specific Src family kinase inhibitor saracatinib (AZD0530) would inhibit tumor cell growth and osteoclast differentiation in the tumor-bone interface, thus providing a new approach for advanced prostate cancer. saracatinib 104-111 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 63-66 20484016-7 2010 Phosphorylation of Src, focal adhesion kinase, and P38 kinases was inhibited by saracatinib at the submicromolar range. saracatinib 80-91 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 19-22 20484016-7 2010 Phosphorylation of Src, focal adhesion kinase, and P38 kinases was inhibited by saracatinib at the submicromolar range. saracatinib 80-91 mitogen-activated protein kinase 14 Homo sapiens 51-54 20484016-8 2010 Saracatinib also inhibited the expression and secretion of invasion-related molecules interlukin-8, urokinase-type plasminogen activator, and matrix metalloprotease-9. saracatinib 0-11 plasminogen activator, urokinase Homo sapiens 100-136 20484016-9 2010 Receptor activator of NF-kappaB ligand (RANKL)-induced osteoclastogenesis and signaling were inhibited by saracatinib in both macrophages and PC-3 cells. saracatinib 106-117 TNF superfamily member 11 Homo sapiens 40-45 20367532-6 2010 WHAT THE READER WILL GAIN: Readers will gain an insight into the development of therapeutic Src inhibitors, including dasatinib and saracatinib; an understanding of their effects on prostate cancer cells and the bone microenvironment; and emerging clinical data. saracatinib 132-143 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 92-95 20015594-5 2010 SRC-targeting agents, including dasatinib, saracatinib, and bosutinib, are currently in clinical development for patients with solid tumors. saracatinib 43-54 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 0-3 19775203-2 2010 We investigated the effect of the orally available Src inhibitor saracatinib (AZD0530) on bone turnover in healthy men. saracatinib 65-76 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 51-54 19393585-0 2009 Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. saracatinib 66-73 SRC proto-oncogene, non-receptor tyrosine kinase Rattus norvegicus 52-55 20505783-2 2009 Src regulates HNSCC proliferation and tumor invasion, with the Src-targeted small molecule inhibitor saracatinib displaying potent anti-invasive effects in preclinical studies. saracatinib 101-112 Rous sarcoma oncogene Mus musculus 63-66 20505783-9 2009 These results suggest that inhibition of Src kinase by saracatinib impairs the pro-invasive activity of HNSCC by inhibiting Src substrate phosphorylation important for invadopodia formation and associated matrix metalloprotease activity. saracatinib 55-66 Rous sarcoma oncogene Mus musculus 41-44 20505783-9 2009 These results suggest that inhibition of Src kinase by saracatinib impairs the pro-invasive activity of HNSCC by inhibiting Src substrate phosphorylation important for invadopodia formation and associated matrix metalloprotease activity. saracatinib 55-66 Rous sarcoma oncogene Mus musculus 124-127 19509160-0 2009 Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer. saracatinib 48-55 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 59-62 19509160-1 2009 PURPOSE: To determine the efficacy of AZD0530, an orally active small molecule Src inhibitor, in human pancreatic cancer xenografts and to seek biomarkers predictive of activity. saracatinib 38-45 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 79-82 19509160-4 2009 Baseline gene expression profiles of differently expressed genes in 16 tumors by Affymetrix U133 Plus 2.0 gene array were used to predict AZD0530 sensitivity in an independent group of eight tumors using the K-Top Scoring Pairs (K-TSP) method. saracatinib 138-145 thrombospondin 1 Homo sapiens 231-234 19509160-6 2009 Western blot and/or immunohistochemistry results showed that AZD0530 administration resulted in the down-regulation of Src, FAK, p-FAK, p-paxillin, p-STAT-3, and XIAP in sensitive tumor xenografts compared with control tumors. saracatinib 61-68 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 119-122 19509160-6 2009 Western blot and/or immunohistochemistry results showed that AZD0530 administration resulted in the down-regulation of Src, FAK, p-FAK, p-paxillin, p-STAT-3, and XIAP in sensitive tumor xenografts compared with control tumors. saracatinib 61-68 protein tyrosine kinase 2 Homo sapiens 124-127 19509160-6 2009 Western blot and/or immunohistochemistry results showed that AZD0530 administration resulted in the down-regulation of Src, FAK, p-FAK, p-paxillin, p-STAT-3, and XIAP in sensitive tumor xenografts compared with control tumors. saracatinib 61-68 protein tyrosine kinase 2 Homo sapiens 131-134 19509160-6 2009 Western blot and/or immunohistochemistry results showed that AZD0530 administration resulted in the down-regulation of Src, FAK, p-FAK, p-paxillin, p-STAT-3, and XIAP in sensitive tumor xenografts compared with control tumors. saracatinib 61-68 X-linked inhibitor of apoptosis Homo sapiens 162-166 19509160-10 2009 One gene pair (LRRC19 and IGFBP2) identified by the K-TSP classifier has high predictive power for AZD0530 sensitivity, suggesting the potential for this gene pair as biomarker for pancreatic tumor sensitivity to AZD0530. saracatinib 99-106 leucine rich repeat containing 19 Homo sapiens 15-21 19509160-10 2009 One gene pair (LRRC19 and IGFBP2) identified by the K-TSP classifier has high predictive power for AZD0530 sensitivity, suggesting the potential for this gene pair as biomarker for pancreatic tumor sensitivity to AZD0530. saracatinib 99-106 insulin like growth factor binding protein 2 Homo sapiens 26-32 19509160-10 2009 One gene pair (LRRC19 and IGFBP2) identified by the K-TSP classifier has high predictive power for AZD0530 sensitivity, suggesting the potential for this gene pair as biomarker for pancreatic tumor sensitivity to AZD0530. saracatinib 99-106 thrombospondin 1 Homo sapiens 54-57 19509160-10 2009 One gene pair (LRRC19 and IGFBP2) identified by the K-TSP classifier has high predictive power for AZD0530 sensitivity, suggesting the potential for this gene pair as biomarker for pancreatic tumor sensitivity to AZD0530. saracatinib 213-220 leucine rich repeat containing 19 Homo sapiens 15-21 19509160-10 2009 One gene pair (LRRC19 and IGFBP2) identified by the K-TSP classifier has high predictive power for AZD0530 sensitivity, suggesting the potential for this gene pair as biomarker for pancreatic tumor sensitivity to AZD0530. saracatinib 213-220 insulin like growth factor binding protein 2 Homo sapiens 26-32 19509160-10 2009 One gene pair (LRRC19 and IGFBP2) identified by the K-TSP classifier has high predictive power for AZD0530 sensitivity, suggesting the potential for this gene pair as biomarker for pancreatic tumor sensitivity to AZD0530. saracatinib 213-220 thrombospondin 1 Homo sapiens 54-57 19293266-0 2009 Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer. saracatinib 23-30 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 19293266-0 2009 Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer. saracatinib 23-30 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 43-46 19293266-0 2009 Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer. saracatinib 23-30 protein tyrosine kinase 2 Homo sapiens 47-68 19293266-4 2009 DESIGN: PTC and ATC cells were treated with the oral Src inhibitor, AZD0530, to determine the consequences of Src inhibition using growth and invasion assays. saracatinib 68-75 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 53-56 19293266-7 2009 Instead, we show for the first time that FAK, a critical substrate and effector of Src, is phosphorylated at tyrosine residue 861 (pY861) in PTC and ATC cells, and high levels of phospho-FAK correlate with AZD0530 sensitivity. saracatinib 206-213 protein tyrosine kinase 2 Homo sapiens 41-44 19293266-7 2009 Instead, we show for the first time that FAK, a critical substrate and effector of Src, is phosphorylated at tyrosine residue 861 (pY861) in PTC and ATC cells, and high levels of phospho-FAK correlate with AZD0530 sensitivity. saracatinib 206-213 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 83-86 19393585-1 2009 AZD0530, an orally available Src inhibitor, demonstrated potent antimigratory and anti-invasive effects in vitro, and inhibited metastasis in a murine model of bladder cancer. saracatinib 0-7 Rous sarcoma oncogene Mus musculus 29-32 19393585-3 2009 AZD0530 inhibited tumor growth in 4/10 xenograft models tested and dynamically inhibited in vivo phosphorylation of Src substrates paxillin and FAK in both growth-inhibition-resistant and -sensitive xenografts. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Rattus norvegicus 116-119 19393585-3 2009 AZD0530 inhibited tumor growth in 4/10 xenograft models tested and dynamically inhibited in vivo phosphorylation of Src substrates paxillin and FAK in both growth-inhibition-resistant and -sensitive xenografts. saracatinib 0-7 protein tyrosine kinase 2 Rattus norvegicus 144-147 19451593-0 2009 Combined Src and aromatase inhibition impairs human breast cancer growth in vivo and bypass pathways are activated in AZD0530-resistant tumors. saracatinib 118-125 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 9-12 19451593-6 2009 RESULTS: AZD0530 and anastrozole together increased p27 and caused greater G(1) cell cycle arrest than either drug alone. saracatinib 9-16 interferon alpha inducible protein 27 Homo sapiens 52-55 19451593-8 2009 Combined anastrozole/AZD0530 reduced drug resistance and showed greater antitumor efficacy in vivo with greater Src and epidermal growth factor receptor inhibition and a greater increase in p27 and reduction of Ki-67 than either drug alone, supporting further evaluation of these putative predictors of response to combined Src/aromatase inhibition in vivo. saracatinib 21-28 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 112-115 19451593-8 2009 Combined anastrozole/AZD0530 reduced drug resistance and showed greater antitumor efficacy in vivo with greater Src and epidermal growth factor receptor inhibition and a greater increase in p27 and reduction of Ki-67 than either drug alone, supporting further evaluation of these putative predictors of response to combined Src/aromatase inhibition in vivo. saracatinib 21-28 epidermal growth factor receptor Homo sapiens 120-152 19451593-8 2009 Combined anastrozole/AZD0530 reduced drug resistance and showed greater antitumor efficacy in vivo with greater Src and epidermal growth factor receptor inhibition and a greater increase in p27 and reduction of Ki-67 than either drug alone, supporting further evaluation of these putative predictors of response to combined Src/aromatase inhibition in vivo. saracatinib 21-28 interferon alpha inducible protein 27 Homo sapiens 190-193 19451593-8 2009 Combined anastrozole/AZD0530 reduced drug resistance and showed greater antitumor efficacy in vivo with greater Src and epidermal growth factor receptor inhibition and a greater increase in p27 and reduction of Ki-67 than either drug alone, supporting further evaluation of these putative predictors of response to combined Src/aromatase inhibition in vivo. saracatinib 21-28 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 324-327 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 mitogen-activated protein kinase kinase 7 Homo sapiens 72-75 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 80-109 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 AKT serine/threonine kinase 1 Homo sapiens 117-120 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 mechanistic target of rapamycin kinase Homo sapiens 121-150 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 mitogen-activated protein kinase kinase 7 Homo sapiens 181-184 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 mechanistic target of rapamycin kinase Homo sapiens 186-215 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 mechanistic target of rapamycin kinase Homo sapiens 217-221 19451593-10 2009 AZD0530-resistant tumors showed activation of bypass pathways including MEK and phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin, raising the possibility that MEK, mammalian target of rapamycin (mTOR), or PI3K inhibitors may augment Src inhibitor efficacy. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 255-258 19154462-8 2009 Encouraging results have been obtained in preclinical and clinical studies using Src inhibitors like AZD0530 and dasatinib. saracatinib 101-108 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 81-84 19372577-0 2009 The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts. saracatinib 18-25 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 4-7 19372577-3 2009 Therefore, drugs like AZD0530, designed to inhibit Src activity, could selectively interfere with both tumor and osteoclast activity. saracatinib 22-29 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 51-54 19372577-7 2009 AZD0530 was most effective in inhibiting osteoclast-like cell formation when present at the onset of osteoclastogenesis, suggesting that Src activity is important during the initial phase of osteoclast formation. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 137-140 19372577-8 2009 Formation of active phosphorylated c-Src, which was highly present in osteoclast-like cells in cocultures and in peripheral blood mononuclear cell monocultures, was significantly reduced by AZD0530. saracatinib 190-197 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 35-40 18409068-3 2009 This study aimed to determine the validity of invasion-related biomarkers of activity for AZD0530, a potent Src inhibitor currently in clinical development. saracatinib 90-97 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 108-111 18409068-9 2009 AZD0530 inhibited tumor growth in a manner independent of dose and inhibited phosphorylation of FAK and paxillin in a dose-dependent manner in a Calu-6 xenograft model. saracatinib 0-7 protein tyrosine kinase 2 Homo sapiens 96-99 18409068-9 2009 AZD0530 inhibited tumor growth in a manner independent of dose and inhibited phosphorylation of FAK and paxillin in a dose-dependent manner in a Calu-6 xenograft model. saracatinib 0-7 paxillin Homo sapiens 104-112 18493848-5 2009 Chronic exposure of both cell types to the Src inhibitor, AZD0530, as a monotherapy resulted in outgrowth of AZD0530-resistant cells, in which Src kinase activity remained suppressed as did their in vitro invasive nature. saracatinib 58-65 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 43-46 18493848-5 2009 Chronic exposure of both cell types to the Src inhibitor, AZD0530, as a monotherapy resulted in outgrowth of AZD0530-resistant cells, in which Src kinase activity remained suppressed as did their in vitro invasive nature. saracatinib 58-65 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 143-146 18493848-5 2009 Chronic exposure of both cell types to the Src inhibitor, AZD0530, as a monotherapy resulted in outgrowth of AZD0530-resistant cells, in which Src kinase activity remained suppressed as did their in vitro invasive nature. saracatinib 109-116 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 43-46 18493848-5 2009 Chronic exposure of both cell types to the Src inhibitor, AZD0530, as a monotherapy resulted in outgrowth of AZD0530-resistant cells, in which Src kinase activity remained suppressed as did their in vitro invasive nature. saracatinib 109-116 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 143-146 18493848-6 2009 Treatment of both MCF7 and T47D cells with AZD0530 in combination with tamoxifen resulted in a reduction of Src activity together with inhibition of focal adhesion kinase phosphorylation and a complete abrogation of their in vitro invasive behaviour. saracatinib 43-50 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 108-111 19240653-0 2009 The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells. saracatinib 18-25 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 4-7 19240653-3 2009 METHODS: This study evaluated the molecular and functional effects of Src inhibitor AZD0530 in human lung cancer cells, by Western blotting and reverse transcription-polymerase chain reaction, and by assays for cell viability, migration, and invasion. saracatinib 84-91 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 70-73 19240653-5 2009 Clinically relevant, submicromolar concentrations of AZD0530 blocked Src and focal adhesion kinase, resulting in significant inhibition of cell migration and Matrigel invasion. saracatinib 53-60 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 69-72 19240653-7 2009 AZD0530 gave a potent and sustained blockage of AKT and enhanced the sensitivity to irradiation. saracatinib 0-7 AKT serine/threonine kinase 1 Homo sapiens 48-51 19098120-6 2009 Phosphorylation of FAK at Tyr(576)/Tyr(577) was inhibited by AZD0530 in a dose-dependent manner both in cell culture and in vitro. saracatinib 61-68 PTK2 protein tyrosine kinase 2 Mus musculus 19-22 19098120-7 2009 However, there was a substantial difference in the ability of AZD0530 to inhibit Src that was constitutively activated in a cellular context (IC(50) = 2.12 muM) compared with the isolated enzyme (IC(50) = 0.14 muM). saracatinib 62-69 Rous sarcoma oncogene Mus musculus 81-84 19216789-4 2009 Here, we investigated the biological effect of the new specific dual Src/Abl kinase inhibitor AZD0530 on Ph+ leukaemic cells. saracatinib 94-101 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 69-72 19216789-13 2009 CONCLUSION: Our results indicate that AZD0530 targets both Src and Bcr-Abl kinase activity and reduces the leukaemic maintenance by Bcr-Abl. saracatinib 38-45 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 59-62 19216789-13 2009 CONCLUSION: Our results indicate that AZD0530 targets both Src and Bcr-Abl kinase activity and reduces the leukaemic maintenance by Bcr-Abl. saracatinib 38-45 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 67-74 19216789-13 2009 CONCLUSION: Our results indicate that AZD0530 targets both Src and Bcr-Abl kinase activity and reduces the leukaemic maintenance by Bcr-Abl. saracatinib 38-45 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 132-139 19060248-5 2009 AZD0530, a selective Src inhibitor, prevented the TPA-induced proliferation of basal keratinocytes both in vivo and in vitro. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 21-24 19117998-7 2009 A Src family kinase (SFK) inhibitor, AZD0530, inhibits androgen-independent growth and migration of the GRP-expressing cell lines, and blocks the nuclear translocation of AR, indicating the involvement of SFK in the aberrant activation of AR and demonstrating the potential use of SFK inhibitor in the treatment of castration-resistant CaP. saracatinib 37-44 gastrin releasing peptide Homo sapiens 104-107 19060248-9 2009 Thus, Src inhibitors such as AZD0530 may therefore have chemopreventative properties in patients with hyperproliferative epidermal disorders. saracatinib 29-36 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 6-9 19235590-1 2009 We hypothesized that co-targeting the epidermal growth factor receptor (EGFR) and Src with the EGFR inhibitor gefitinib and the Src inhibitor AZD0530 would increase growth inhibition and impede migration. saracatinib 142-149 epidermal growth factor receptor Homo sapiens 38-70 19235590-1 2009 We hypothesized that co-targeting the epidermal growth factor receptor (EGFR) and Src with the EGFR inhibitor gefitinib and the Src inhibitor AZD0530 would increase growth inhibition and impede migration. saracatinib 142-149 epidermal growth factor receptor Homo sapiens 72-76 19235590-1 2009 We hypothesized that co-targeting the epidermal growth factor receptor (EGFR) and Src with the EGFR inhibitor gefitinib and the Src inhibitor AZD0530 would increase growth inhibition and impede migration. saracatinib 142-149 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 128-131 18924149-7 2009 Src activity in both hypoxic and nonhypoxic BxPC3 tumor regions was suppressed when mice were treated with the Src inhibitor AZD0530 (25 mg/kg/day, 5 days), suggesting that both hypoxic and normoxic tumor regions are accessible to pharmacological Src inhibition. saracatinib 125-132 Rous sarcoma oncogene Mus musculus 0-3 18924149-7 2009 Src activity in both hypoxic and nonhypoxic BxPC3 tumor regions was suppressed when mice were treated with the Src inhibitor AZD0530 (25 mg/kg/day, 5 days), suggesting that both hypoxic and normoxic tumor regions are accessible to pharmacological Src inhibition. saracatinib 125-132 Rous sarcoma oncogene Mus musculus 111-114 18924149-7 2009 Src activity in both hypoxic and nonhypoxic BxPC3 tumor regions was suppressed when mice were treated with the Src inhibitor AZD0530 (25 mg/kg/day, 5 days), suggesting that both hypoxic and normoxic tumor regions are accessible to pharmacological Src inhibition. saracatinib 125-132 Rous sarcoma oncogene Mus musculus 111-114 18613032-10 2009 The selective Src inhibitor, AZD0530, was found to be effective in blocking both cell invasion and anchorage-independent proliferation. saracatinib 29-36 Rous sarcoma oncogene Mus musculus 14-17 19117998-7 2009 A Src family kinase (SFK) inhibitor, AZD0530, inhibits androgen-independent growth and migration of the GRP-expressing cell lines, and blocks the nuclear translocation of AR, indicating the involvement of SFK in the aberrant activation of AR and demonstrating the potential use of SFK inhibitor in the treatment of castration-resistant CaP. saracatinib 37-44 androgen receptor Homo sapiens 171-173 19117998-7 2009 A Src family kinase (SFK) inhibitor, AZD0530, inhibits androgen-independent growth and migration of the GRP-expressing cell lines, and blocks the nuclear translocation of AR, indicating the involvement of SFK in the aberrant activation of AR and demonstrating the potential use of SFK inhibitor in the treatment of castration-resistant CaP. saracatinib 37-44 androgen receptor Homo sapiens 239-241 19117998-8 2009 In vivo studies have shown that AZD0530 profoundly inhibits tumor metastasis in severe combined immunodeficient mice implanted with GRP-autocrine LNCaP cells. saracatinib 32-39 gastrin releasing peptide Mus musculus 132-135 18679417-0 2008 Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. saracatinib 85-92 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 0-3 18679417-3 2008 We sought to investigate the Src-mediated oncogenic pathways and tumor biology using AZD0530, a novel Src family kinase/Abl dual-kinase inhibitor that is entering phase II clinical trials. saracatinib 85-92 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 29-32 18679417-3 2008 We sought to investigate the Src-mediated oncogenic pathways and tumor biology using AZD0530, a novel Src family kinase/Abl dual-kinase inhibitor that is entering phase II clinical trials. saracatinib 85-92 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 102-105 18679417-3 2008 We sought to investigate the Src-mediated oncogenic pathways and tumor biology using AZD0530, a novel Src family kinase/Abl dual-kinase inhibitor that is entering phase II clinical trials. saracatinib 85-92 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 120-123 18679417-5 2008 Furthermore, Src activation is inhibited by AZD0530 in a rapid and dose-dependent manner. saracatinib 44-51 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 13-16 17394086-5 2007 Inhibition of Src activity using the Src/Abl inhibitor AZD0530 reduced FAK activity, suppressed cell spreading on matrix-coated surfaces and significantly inhibited cell migration. saracatinib 55-62 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 14-17 17918184-7 2008 Treatment with the dual specific Abl/c-Src kinase inhibitor AZD0530 significantly reduces the growth inhibitory effect of high EGF concentrations, signifying that EGFR induced IRF-1 is responsible for the observed growth inhibition. saracatinib 60-67 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 33-36 17918184-7 2008 Treatment with the dual specific Abl/c-Src kinase inhibitor AZD0530 significantly reduces the growth inhibitory effect of high EGF concentrations, signifying that EGFR induced IRF-1 is responsible for the observed growth inhibition. saracatinib 60-67 C-terminal Src kinase Homo sapiens 37-49 17918184-7 2008 Treatment with the dual specific Abl/c-Src kinase inhibitor AZD0530 significantly reduces the growth inhibitory effect of high EGF concentrations, signifying that EGFR induced IRF-1 is responsible for the observed growth inhibition. saracatinib 60-67 epidermal growth factor receptor Homo sapiens 163-167 17918184-7 2008 Treatment with the dual specific Abl/c-Src kinase inhibitor AZD0530 significantly reduces the growth inhibitory effect of high EGF concentrations, signifying that EGFR induced IRF-1 is responsible for the observed growth inhibition. saracatinib 60-67 interferon regulatory factor 1 Homo sapiens 176-181 18594017-7 2008 RESULTS: Here, we show that inhibition of PLCgamma-1 or c-Src with the PLC inhibitor U73122 or the Src family inhibitor AZD0530 or using dominant-negative constructs attenuated epidermal growth factor (EGF)-stimulated HNSCC invasion. saracatinib 120-127 phospholipase C gamma 1 Homo sapiens 42-52 18594017-7 2008 RESULTS: Here, we show that inhibition of PLCgamma-1 or c-Src with the PLC inhibitor U73122 or the Src family inhibitor AZD0530 or using dominant-negative constructs attenuated epidermal growth factor (EGF)-stimulated HNSCC invasion. saracatinib 120-127 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 56-61 18594017-7 2008 RESULTS: Here, we show that inhibition of PLCgamma-1 or c-Src with the PLC inhibitor U73122 or the Src family inhibitor AZD0530 or using dominant-negative constructs attenuated epidermal growth factor (EGF)-stimulated HNSCC invasion. saracatinib 120-127 heparan sulfate proteoglycan 2 Homo sapiens 42-45 18594017-7 2008 RESULTS: Here, we show that inhibition of PLCgamma-1 or c-Src with the PLC inhibitor U73122 or the Src family inhibitor AZD0530 or using dominant-negative constructs attenuated epidermal growth factor (EGF)-stimulated HNSCC invasion. saracatinib 120-127 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 58-61 18381431-3 2008 Microarray analyses showed that Id family genes were among the most highly down-regulated by incubation of A549 lung carcinoma cells with the small-molecule Src inhibitor AZD0530. saracatinib 171-178 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 157-160 18381431-6 2008 PP2, AZD0530, and dominant-negative Src abrogated Id1 promoter activity, which was induced by constitutively active Src. saracatinib 5-12 inhibitor of DNA binding 1, HLH protein Homo sapiens 50-53 17704648-2 2007 We here demonstrate that three newly developed dual selective Src/Abl kinase inhibitors (SrcK-I) (AZM559756, AZD0530 and AZD0424) are able to induce apoptosis and cell cycle arrest in BCR-ABL, c-KIT and platelet-derived growth factor-negative lymphoma cell lines. saracatinib 109-116 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 184-191 17704648-2 2007 We here demonstrate that three newly developed dual selective Src/Abl kinase inhibitors (SrcK-I) (AZM559756, AZD0530 and AZD0424) are able to induce apoptosis and cell cycle arrest in BCR-ABL, c-KIT and platelet-derived growth factor-negative lymphoma cell lines. saracatinib 109-116 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 193-198 17394086-5 2007 Inhibition of Src activity using the Src/Abl inhibitor AZD0530 reduced FAK activity, suppressed cell spreading on matrix-coated surfaces and significantly inhibited cell migration. saracatinib 55-62 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 37-40 17394086-5 2007 Inhibition of Src activity using the Src/Abl inhibitor AZD0530 reduced FAK activity, suppressed cell spreading on matrix-coated surfaces and significantly inhibited cell migration. saracatinib 55-62 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 41-44 17394086-5 2007 Inhibition of Src activity using the Src/Abl inhibitor AZD0530 reduced FAK activity, suppressed cell spreading on matrix-coated surfaces and significantly inhibited cell migration. saracatinib 55-62 protein tyrosine kinase 2 Homo sapiens 71-74 17064066-4 2006 N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. saracatinib 122-129 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 140-145 17259559-6 2006 Using the dual specific Src/Abl kinase inhibitor, AZD0530, we have highlighted a central role for Src kinase in promoting the invasive phenotype that accompanies both anti-hormone and anti-growth factor resistance. saracatinib 50-57 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 98-101 17172405-6 2006 A c-Src inhibitor, AZD0530, was used to analyze the biological effects of pharmacologically inhibiting c-Src kinase activity. saracatinib 19-26 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 2-7 17172405-6 2006 A c-Src inhibitor, AZD0530, was used to analyze the biological effects of pharmacologically inhibiting c-Src kinase activity. saracatinib 19-26 C-terminal Src kinase Homo sapiens 103-115 17173196-10 2006 Compared with that in the control group, the levels of AIF mRNA expression were significantly higher in the groups of H8h and H12h (0.52+/-0.04 and 0.85+/-0.10), indicating that this effect was time-dependent. saracatinib 118-121 apoptosis inducing factor mitochondria associated 1 Homo sapiens 55-58 17173196-13 2006 Compared with that in the control group, the levels of AIF protein expression were significantly higher in the groups of H8h and H12h (2.07+/-0.15 and 3.12+/-0.19). saracatinib 121-124 apoptosis inducing factor mitochondria associated 1 Homo sapiens 55-58 17173196-14 2006 The AIF protein expression was increased further in the groups of H8h/R (4.57+/-0.25) and H12h/R (5.71+/-0.27). saracatinib 66-69 apoptosis inducing factor mitochondria associated 1 Homo sapiens 4-7 17064066-4 2006 N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. saracatinib 122-129 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 150-153 17064066-6 2006 AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily. saracatinib 0-7 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 51-56 16333527-7 2006 Treatment of TamR cells with the novel Src inhibitor, AZD0530, significantly reduced the amount of activated Src detectable in both cell types whilst having no effect on total Src levels. saracatinib 54-61 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 39-42 16333527-7 2006 Treatment of TamR cells with the novel Src inhibitor, AZD0530, significantly reduced the amount of activated Src detectable in both cell types whilst having no effect on total Src levels. saracatinib 54-61 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 109-112 16333527-7 2006 Treatment of TamR cells with the novel Src inhibitor, AZD0530, significantly reduced the amount of activated Src detectable in both cell types whilst having no effect on total Src levels. saracatinib 54-61 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 109-112 16333527-8 2006 AZD0530 significantly suppressed the motile and invasive nature of TamR cells in vitro, reduced basal levels of activated focal adhesion kinase (FAK) and paxillin and promoted elongation of focal adhesions. saracatinib 0-7 protein tyrosine kinase 2 Homo sapiens 122-143 16333527-8 2006 AZD0530 significantly suppressed the motile and invasive nature of TamR cells in vitro, reduced basal levels of activated focal adhesion kinase (FAK) and paxillin and promoted elongation of focal adhesions. saracatinib 0-7 protein tyrosine kinase 2 Homo sapiens 145-148 16113095-5 2005 Candidate drugs for several of these targets are currently being evaluated; for example, the prenylation inhibitor AZD3409, a mimetic of the CAAX box of K-Ras, inhibits protein farnesyl and geranylgeranyl tranferases and a novel, selective, orally active Src kinase inhibitor AZD0530 have entered Phase I clinical trials and may have utility in breast cancer therapy. saracatinib 276-283 KRAS proto-oncogene, GTPase Homo sapiens 153-158