PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32783069-8 2021 RESULTS: Stimulation with IL-17A induced STAT3 phosphorylation, which was inhibited by the pretreatment with JAK2 inhibitor AZD1480 or JAK1/3 inhibitor tofacitinib. AZD 1480 124-131 interleukin 17A Homo sapiens 26-32 34685476-2 2021 In the present study, we identified increased isoprenaline-induced aa-nat expression and nocturnal AANAT activity in the pineal glands in response to the silencing of the signal transducer and activator of transcription 3 (STAT3) with siRNA or STAT3 inhibitors WP1066 and AZD1480. AZD 1480 272-279 aralkylamine N-acetyltransferase Rattus norvegicus 99-104 34685476-2 2021 In the present study, we identified increased isoprenaline-induced aa-nat expression and nocturnal AANAT activity in the pineal glands in response to the silencing of the signal transducer and activator of transcription 3 (STAT3) with siRNA or STAT3 inhibitors WP1066 and AZD1480. AZD 1480 272-279 signal transducer and activator of transcription 3 Rattus norvegicus 244-249 35207737-8 2022 Since Janus kinases2 (JAK2) was considered as one of the down-stream kinases under IL4Ralpha and IL13Ralpha1 complex, the same kinds of experiments were performed in SNU308 cells treated with AZD1480, Janus-associated kinases2 (JAK2) inhibitor, to demonstrate the cytotoxic effect of AZD1480 in SNU308 cells. AZD 1480 192-199 Janus kinase 2 Homo sapiens 22-26 35207737-8 2022 Since Janus kinases2 (JAK2) was considered as one of the down-stream kinases under IL4Ralpha and IL13Ralpha1 complex, the same kinds of experiments were performed in SNU308 cells treated with AZD1480, Janus-associated kinases2 (JAK2) inhibitor, to demonstrate the cytotoxic effect of AZD1480 in SNU308 cells. AZD 1480 284-291 Janus kinase 2 Homo sapiens 22-26 35207737-12 2022 Then, we found that knockdown of IL4Ralpha or IL13Ralpha1 decreased viability and induced apoptosis in SNU308 cells via activation of FOXO3 and similarly, AZD1480 decreased viability and induced apoptosis in SNU308 cells with dose dependent manner. AZD 1480 155-162 interleukin 4 receptor Homo sapiens 33-42 35207737-12 2022 Then, we found that knockdown of IL4Ralpha or IL13Ralpha1 decreased viability and induced apoptosis in SNU308 cells via activation of FOXO3 and similarly, AZD1480 decreased viability and induced apoptosis in SNU308 cells with dose dependent manner. AZD 1480 155-162 interleukin 13 receptor subunit alpha 1 Homo sapiens 46-57 34904774-4 2022 The JAK2 inhibitor AZD-1480 was introduced to explore the specific mechanism by which IVM regulates glycolysis and autophagy. AZD 1480 19-27 Janus kinase 2 Rattus norvegicus 4-8 32783069-8 2021 RESULTS: Stimulation with IL-17A induced STAT3 phosphorylation, which was inhibited by the pretreatment with JAK2 inhibitor AZD1480 or JAK1/3 inhibitor tofacitinib. AZD 1480 124-131 signal transducer and activator of transcription 3 Homo sapiens 41-46 32783069-8 2021 RESULTS: Stimulation with IL-17A induced STAT3 phosphorylation, which was inhibited by the pretreatment with JAK2 inhibitor AZD1480 or JAK1/3 inhibitor tofacitinib. AZD 1480 124-131 Janus kinase 2 Homo sapiens 109-113 33102814-9 2020 Furthermore, while JAK2 inhibition leads to decreased viability in SeAx cells (IC50 of 9.98 and 29.15 muM for AZD1480 and ruxolitinib respectively), both JAK1 and JAK3 do not. AZD 1480 110-117 Janus kinase 2 Homo sapiens 19-23 30007232-15 2018 In contrast, AZD1480, a JAK2 inhibitor, abolished this SN-EPO effect. AZD 1480 13-20 Janus kinase 2 Mus musculus 24-28 30604628-7 2019 In addition, inhibiting Janus activated kinase (JAK) 2 by either siRNA or a selective pharmacological inhibitor, AZD1480-but not a JAK1/JAK3 selective inhibitor, tofacitinib-also significantly reduced this IL-17A-induced fibrogenic response. AZD 1480 113-120 interleukin 17A Homo sapiens 206-212 32768575-10 2020 Inhibition of the IL-6/JAK/STAT3 pathway with the JAK1/2 specific inhibitor, AZD1480, reversed the associated increase of IL-6. AZD 1480 77-84 interleukin 6 Homo sapiens 18-22 32768575-10 2020 Inhibition of the IL-6/JAK/STAT3 pathway with the JAK1/2 specific inhibitor, AZD1480, reversed the associated increase of IL-6. AZD 1480 77-84 signal transducer and activator of transcription 3 Homo sapiens 27-32 32768575-10 2020 Inhibition of the IL-6/JAK/STAT3 pathway with the JAK1/2 specific inhibitor, AZD1480, reversed the associated increase of IL-6. AZD 1480 77-84 Janus kinase 1 Homo sapiens 50-56 32768575-10 2020 Inhibition of the IL-6/JAK/STAT3 pathway with the JAK1/2 specific inhibitor, AZD1480, reversed the associated increase of IL-6. AZD 1480 77-84 interleukin 6 Homo sapiens 122-126 32144852-7 2020 Furthermore, treatment of JAK2 clinical medicine AZD1480 to ESCC cells showed similar tendency with Lico B. AZD 1480 49-56 Janus kinase 2 Homo sapiens 26-30 32005799-5 2020 Interruption of IL-6/JAK/STAT3 pathway by a JAK inhibitor AZD1480 reverses the pro-metastatic effect of sevoflurane and the associated increase of both activated STAT3 and infiltrated CD11b+ cells in 4T1 model. AZD 1480 58-65 interleukin 6 Homo sapiens 16-20 32005799-5 2020 Interruption of IL-6/JAK/STAT3 pathway by a JAK inhibitor AZD1480 reverses the pro-metastatic effect of sevoflurane and the associated increase of both activated STAT3 and infiltrated CD11b+ cells in 4T1 model. AZD 1480 58-65 signal transducer and activator of transcription 3 Homo sapiens 25-30 32005799-5 2020 Interruption of IL-6/JAK/STAT3 pathway by a JAK inhibitor AZD1480 reverses the pro-metastatic effect of sevoflurane and the associated increase of both activated STAT3 and infiltrated CD11b+ cells in 4T1 model. AZD 1480 58-65 signal transducer and activator of transcription 3 Homo sapiens 162-167 32005799-5 2020 Interruption of IL-6/JAK/STAT3 pathway by a JAK inhibitor AZD1480 reverses the pro-metastatic effect of sevoflurane and the associated increase of both activated STAT3 and infiltrated CD11b+ cells in 4T1 model. AZD 1480 58-65 integrin subunit alpha M Homo sapiens 184-189 31467427-3 2019 In this study, using lipopolysaccharide (LPS) inhalation plus mechanical ventilation as VILI mouse model, we found that the administration of JAK2 inhibitor AZD1480 markedly attenuated lung destruction, diminished protein leakage, and inhibited cytokine release. AZD 1480 157-164 Janus kinase 2 Mus musculus 142-146 31467427-4 2019 In addition, when mouse macrophage-like RAW 264.7 cells were exposed to LPS and cyclic stretch (CS), AZD1480 prevented cell autophagy, reduced apoptosis, and suppressed lactate dehydrogenase release by downregulating JAK2/STAT1 phosphorylation levels and inducing HMGB1 translocation from the nucleus to the cytoplasm. AZD 1480 101-108 Janus kinase 2 Mus musculus 217-221 31467427-4 2019 In addition, when mouse macrophage-like RAW 264.7 cells were exposed to LPS and cyclic stretch (CS), AZD1480 prevented cell autophagy, reduced apoptosis, and suppressed lactate dehydrogenase release by downregulating JAK2/STAT1 phosphorylation levels and inducing HMGB1 translocation from the nucleus to the cytoplasm. AZD 1480 101-108 signal transducer and activator of transcription 1 Mus musculus 222-227 31467427-4 2019 In addition, when mouse macrophage-like RAW 264.7 cells were exposed to LPS and cyclic stretch (CS), AZD1480 prevented cell autophagy, reduced apoptosis, and suppressed lactate dehydrogenase release by downregulating JAK2/STAT1 phosphorylation levels and inducing HMGB1 translocation from the nucleus to the cytoplasm. AZD 1480 101-108 high mobility group box 1 Mus musculus 264-269 30015925-8 2018 The use of the JAK2 inhibitor, AZD-1480, attenuated the suppressive effects of LKB1 overexpression on the growth, metastasis and self-renewal ability of the GBC cells, which further demonstrated that JAK/STAT3 was involved in the LKB1-induced suppression of GBC cell growth, metastasis and self-renewal ability. AZD 1480 31-39 Janus kinase 2 Homo sapiens 15-19 30015925-8 2018 The use of the JAK2 inhibitor, AZD-1480, attenuated the suppressive effects of LKB1 overexpression on the growth, metastasis and self-renewal ability of the GBC cells, which further demonstrated that JAK/STAT3 was involved in the LKB1-induced suppression of GBC cell growth, metastasis and self-renewal ability. AZD 1480 31-39 serine/threonine kinase 11 Homo sapiens 79-83 30015925-8 2018 The use of the JAK2 inhibitor, AZD-1480, attenuated the suppressive effects of LKB1 overexpression on the growth, metastasis and self-renewal ability of the GBC cells, which further demonstrated that JAK/STAT3 was involved in the LKB1-induced suppression of GBC cell growth, metastasis and self-renewal ability. AZD 1480 31-39 signal transducer and activator of transcription 3 Homo sapiens 204-209 30015925-8 2018 The use of the JAK2 inhibitor, AZD-1480, attenuated the suppressive effects of LKB1 overexpression on the growth, metastasis and self-renewal ability of the GBC cells, which further demonstrated that JAK/STAT3 was involved in the LKB1-induced suppression of GBC cell growth, metastasis and self-renewal ability. AZD 1480 31-39 serine/threonine kinase 11 Homo sapiens 230-234 30007232-15 2018 In contrast, AZD1480, a JAK2 inhibitor, abolished this SN-EPO effect. AZD 1480 13-20 erythropoietin Mus musculus 55-61 30038287-8 2018 Further work demonstrated that the combination of PD98059 with AZD1480 could reverse the effects of PEAK1-induced EMT, cell migration and invasion. AZD 1480 63-70 pseudopodium enriched atypical kinase 1 Homo sapiens 100-105 29722127-4 2018 Functional analysis was conducted by siRNA-mediated CD90, Gli1 and Gli3 gene knockdown, SHH treatment and application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody in CD90+ liver cancer stem cells, followed by cell proliferation, migration, sphere formation and tumorigenicity assays. AZD 1480 140-147 Janus kinase 2 Homo sapiens 125-129 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 Janus kinase 2 Homo sapiens 19-23 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 Thy-1 cell surface antigen Homo sapiens 83-87 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 sonic hedgehog signaling molecule Homo sapiens 92-95 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 GLI family zinc finger 1 Homo sapiens 96-99 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 interleukin 6 Homo sapiens 164-167 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 Janus kinase 2 Homo sapiens 168-172 29722127-8 2018 Application of the JAK2 inhibitor AZD1480 and IL6 neutralizing antibody showed the CD90 and SHH/Gli-regulated liver cancer stem cell functions were mediated by the IL6/JAK2/STAT3 pathway. AZD 1480 34-41 signal transducer and activator of transcription 3 Homo sapiens 173-178 29102603-7 2017 Moreover, the expression levels of p-JAK2 and p-STAT3 were significantly increased in the cortex after SAH induction and were further increased by EPO treatment; in addition, the p-JAK2 inhibitor AZD1480 impaired the protective effect of EPO against SAH-induced EBI in vivo. AZD 1480 196-203 Janus kinase 2 Homo sapiens 37-41 29345196-10 2018 Hyperactivation of pSTAT3 and inflammation were rescued by AZD1480, a JAK1/2 inhibitor. AZD 1480 59-66 Janus kinase 1 Mus musculus 70-76 29102603-7 2017 Moreover, the expression levels of p-JAK2 and p-STAT3 were significantly increased in the cortex after SAH induction and were further increased by EPO treatment; in addition, the p-JAK2 inhibitor AZD1480 impaired the protective effect of EPO against SAH-induced EBI in vivo. AZD 1480 196-203 erythropoietin Homo sapiens 238-241 29102603-7 2017 Moreover, the expression levels of p-JAK2 and p-STAT3 were significantly increased in the cortex after SAH induction and were further increased by EPO treatment; in addition, the p-JAK2 inhibitor AZD1480 impaired the protective effect of EPO against SAH-induced EBI in vivo. AZD 1480 196-203 signal transducer and activator of transcription 3 Homo sapiens 48-53 29102603-7 2017 Moreover, the expression levels of p-JAK2 and p-STAT3 were significantly increased in the cortex after SAH induction and were further increased by EPO treatment; in addition, the p-JAK2 inhibitor AZD1480 impaired the protective effect of EPO against SAH-induced EBI in vivo. AZD 1480 196-203 erythropoietin Homo sapiens 147-150 29102603-7 2017 Moreover, the expression levels of p-JAK2 and p-STAT3 were significantly increased in the cortex after SAH induction and were further increased by EPO treatment; in addition, the p-JAK2 inhibitor AZD1480 impaired the protective effect of EPO against SAH-induced EBI in vivo. AZD 1480 196-203 Janus kinase 2 Homo sapiens 181-185 29312610-0 2017 Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480. AZD 1480 84-91 ALK receptor tyrosine kinase Homo sapiens 30-33 29312610-0 2017 Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480. AZD 1480 84-91 leukocyte receptor tyrosine kinase Homo sapiens 35-38 29312610-0 2017 Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480. AZD 1480 84-91 ret proto-oncogene Homo sapiens 46-49 29312610-3 2017 Here, we searched for novel targets of AZD1480, an inhibitor of JAK2 kinase that recently failed phase two cancer clinical trials due to a lack of activity. AZD 1480 39-46 Janus kinase 2 Homo sapiens 64-68 29312610-5 2017 We demonstrate that AZD1480 inhibits ALK, LTK, FGFR1-3, RET and TRKA-C kinases and uncover a physical basis of this specificity. AZD 1480 20-27 ALK receptor tyrosine kinase Homo sapiens 37-40 29312610-5 2017 We demonstrate that AZD1480 inhibits ALK, LTK, FGFR1-3, RET and TRKA-C kinases and uncover a physical basis of this specificity. AZD 1480 20-27 leukocyte receptor tyrosine kinase Homo sapiens 42-45 29312610-5 2017 We demonstrate that AZD1480 inhibits ALK, LTK, FGFR1-3, RET and TRKA-C kinases and uncover a physical basis of this specificity. AZD 1480 20-27 fibroblast growth factor receptor 1 Homo sapiens 47-54 29312610-5 2017 We demonstrate that AZD1480 inhibits ALK, LTK, FGFR1-3, RET and TRKA-C kinases and uncover a physical basis of this specificity. AZD 1480 20-27 ret proto-oncogene Homo sapiens 56-59 29228586-7 2017 Hypoxia-induced p-STAT3 increased the mRNA transcription of ICAM-1, which we could inhibit with the STAT3 inhibitor AZD1480. AZD 1480 116-123 signal transducer and activator of transcription 3 Mus musculus 18-23 28960447-0 2017 JAK1/2 Inhibitors AZD1480 and CYT387 Inhibit Canine B-Cell Lymphoma Growth by Increasing Apoptosis and Disrupting Cell Proliferation. AZD 1480 18-25 Janus kinase 1 Canis lupus familiaris 0-4 28960447-4 2017 AZD1480 and CYT387 are novel JAK1/2 inhibitors that have been used in clinical trials for treating various hematologic cancers in humans. AZD 1480 0-7 Janus kinase 1 Homo sapiens 29-35 28960447-6 2017 HYPOTHESIS/OBJECTIVES: We hypothesize that JAK1/2 inhibitors AZD1480 and CYT387 can effectively inhibit growth of canine DLBCL in vitro. AZD 1480 61-68 Janus kinase 1 Canis lupus familiaris 43-47 29228586-7 2017 Hypoxia-induced p-STAT3 increased the mRNA transcription of ICAM-1, which we could inhibit with the STAT3 inhibitor AZD1480. AZD 1480 116-123 signal transducer and activator of transcription 3 Mus musculus 100-105 29228586-7 2017 Hypoxia-induced p-STAT3 increased the mRNA transcription of ICAM-1, which we could inhibit with the STAT3 inhibitor AZD1480. AZD 1480 116-123 intercellular adhesion molecule 1 Mus musculus 60-66 26510863-7 2015 The strongest effects were observed by suppressing JAK1/2 signaling with AZD1480. AZD 1480 73-80 Janus kinase 1 Bos taurus 51-55 28039266-8 2017 Transient blockade of CD11b+ cell expansion using a JAK 1/2 Inhibitor (AZD1480) impaired mobilization of these cells and was associated with a reduction in tumor volume, maintenance of a low-grade tumor phenotype, and prolongation in survival.Conclusions: We demonstrate that impaired recruitment of CD11b+ myeloid cells with a JAK1/2 inhibitor inhibits glioma progression in vivo and prolongs survival in a murine glioma model. AZD 1480 71-78 integrin subunit alpha M Homo sapiens 22-27 28039266-8 2017 Transient blockade of CD11b+ cell expansion using a JAK 1/2 Inhibitor (AZD1480) impaired mobilization of these cells and was associated with a reduction in tumor volume, maintenance of a low-grade tumor phenotype, and prolongation in survival.Conclusions: We demonstrate that impaired recruitment of CD11b+ myeloid cells with a JAK1/2 inhibitor inhibits glioma progression in vivo and prolongs survival in a murine glioma model. AZD 1480 71-78 Janus kinase 1 Homo sapiens 52-59 28039266-8 2017 Transient blockade of CD11b+ cell expansion using a JAK 1/2 Inhibitor (AZD1480) impaired mobilization of these cells and was associated with a reduction in tumor volume, maintenance of a low-grade tumor phenotype, and prolongation in survival.Conclusions: We demonstrate that impaired recruitment of CD11b+ myeloid cells with a JAK1/2 inhibitor inhibits glioma progression in vivo and prolongs survival in a murine glioma model. AZD 1480 71-78 integrin subunit alpha M Homo sapiens 300-305 28039266-8 2017 Transient blockade of CD11b+ cell expansion using a JAK 1/2 Inhibitor (AZD1480) impaired mobilization of these cells and was associated with a reduction in tumor volume, maintenance of a low-grade tumor phenotype, and prolongation in survival.Conclusions: We demonstrate that impaired recruitment of CD11b+ myeloid cells with a JAK1/2 inhibitor inhibits glioma progression in vivo and prolongs survival in a murine glioma model. AZD 1480 71-78 Janus kinase 1 Homo sapiens 328-334 27147665-6 2016 In vitro, alpha-SYN exposure activated the JAK/STAT pathway in microglia and macrophages, and treatment with AZD1480 inhibited alpha-SYN-induced major histocompatibility complex Class II and inflammatory gene expression in microglia and macrophages by reducing STAT1 and STAT3 activation. AZD 1480 109-116 Janus kinase 1 Rattus norvegicus 43-46 27147665-6 2016 In vitro, alpha-SYN exposure activated the JAK/STAT pathway in microglia and macrophages, and treatment with AZD1480 inhibited alpha-SYN-induced major histocompatibility complex Class II and inflammatory gene expression in microglia and macrophages by reducing STAT1 and STAT3 activation. AZD 1480 109-116 signal transducer and activator of transcription 1 Rattus norvegicus 261-266 27147665-6 2016 In vitro, alpha-SYN exposure activated the JAK/STAT pathway in microglia and macrophages, and treatment with AZD1480 inhibited alpha-SYN-induced major histocompatibility complex Class II and inflammatory gene expression in microglia and macrophages by reducing STAT1 and STAT3 activation. AZD 1480 109-116 signal transducer and activator of transcription 3 Rattus norvegicus 271-276 27147665-8 2016 AZD1480 treatment inhibited alpha-SYN-induced neuroinflammation by suppressing microglial activation, macrophage and CD4(+) T-cell infiltration and production of proinflammatory cytokines/chemokines. AZD 1480 0-7 Cd4 molecule Rattus norvegicus 117-120 27147665-13 2016 Using an alpha-SYN overexpression PD model, we demonstrate a beneficial therapeutic effect of AZD1480, a specific inhibitor of JAK1/2, in suppressing neuroinflammation and neurodegeneration. AZD 1480 94-101 Janus kinase 1 Rattus norvegicus 127-133 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 discoidin domain receptor tyrosine kinase 2 Homo sapiens 63-67 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 insulin like growth factor 1 receptor Homo sapiens 69-74 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 fms related receptor tyrosine kinase 3 Homo sapiens 76-80 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 neurotrophic receptor tyrosine kinase 1 Homo sapiens 82-86 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 fms related receptor tyrosine kinase 4 Homo sapiens 88-92 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 94-97 26494904-8 2016 This was most extensive in SU5402 and AZD1480, which inhibited DDR2, IGF1R, FLT3, TRKA, FLT4, ABL and JAK3 with efficiencies similar to or greater than those for FGFR. AZD 1480 38-45 Janus kinase 3 Homo sapiens 102-106 28292965-6 2017 The JAK1/JAK2 inhibitor AZD1480 blocked the effect of cytokines on mouse and human beta-cells by inhibiting MHC class I upregulation. AZD 1480 24-31 Janus kinase 1 Mus musculus 4-8 28292965-6 2017 The JAK1/JAK2 inhibitor AZD1480 blocked the effect of cytokines on mouse and human beta-cells by inhibiting MHC class I upregulation. AZD 1480 24-31 Janus kinase 2 Mus musculus 9-13 27976373-9 2017 AZD1480, an ATP-competitive JAK2 inhibitor, abrogated the observed TAM-mediated MM cell survival, and partially inhibited resistance to bortezomib. AZD 1480 0-7 Janus kinase 2 Mus musculus 28-32 27976373-12 2017 As a result of TAM-induced activation of the STAT3 pathway, 5T33MM cells are sensitized to AZD1480 treatment. AZD 1480 91-98 signal transducer and activator of transcription 3 Mus musculus 45-50 25704089-0 2015 The JAK2 inhibitor AZD1480 inhibits hepatitis A virus replication in Huh7 cells. AZD 1480 19-26 Janus kinase 2 Homo sapiens 4-8 26419724-3 2015 Using in vitro drug screening, we identified 211 amino-acid substitutions conferring resistance to ruxolitinib (INCB018424) and cross-resistance to the JAK2 inhibitors AZD1480, CYT-387 and lestaurtinib. AZD 1480 168-175 Janus kinase 2 Homo sapiens 152-156 25646015-8 2015 AZD1480 treatment inhibited STAT3 phosphorylation and DNA binding, and migration and adhesion of cultured ovarian carcinoma cells and ovarian tumor growth rate, volume, and ascites production in mice. AZD 1480 0-7 signal transducer and activator of transcription 3 Mus musculus 28-33 25704089-1 2015 The JAK2 inhibitor AZD1480 has been reported to inhibit La protein expression. AZD 1480 19-26 Janus kinase 2 Homo sapiens 4-8 25704089-6 2015 Furthermore, AZD1480 inhibited the expression of phosphorylated-(Tyr-705)-signal transducer and activator of transcription 3 (STAT3) and La in Huh7 cells. AZD 1480 13-20 signal transducer and activator of transcription 3 Homo sapiens 74-124 25704089-6 2015 Furthermore, AZD1480 inhibited the expression of phosphorylated-(Tyr-705)-signal transducer and activator of transcription 3 (STAT3) and La in Huh7 cells. AZD 1480 13-20 signal transducer and activator of transcription 3 Homo sapiens 126-131 25810010-2 2015 AZD1480, an orally active pharmacologic inhibitor of JAK1/JAK2, has been tested in several cancer models. AZD 1480 0-7 Janus kinase 1 Homo sapiens 53-57 25810010-2 2015 AZD1480, an orally active pharmacologic inhibitor of JAK1/JAK2, has been tested in several cancer models. AZD 1480 0-7 Janus kinase 2 Homo sapiens 58-62 25504635-2 2015 The purpose of this study was to assess the preclinical efficacy of the JAK1/2 inhibitor AZD1480, both as a single agent and in combination with the MEK inhibitor selumetinib, against JAK-mutated patient-derived xenografts. AZD 1480 89-96 Janus kinase 1 Homo sapiens 72-76 25530567-0 2015 A phase I, open-label, multi-center study of the JAK2 inhibitor AZD1480 in patients with myelofibrosis. AZD 1480 64-71 Janus kinase 2 Homo sapiens 49-53 25216185-0 2014 AZD1480, a JAK inhibitor, inhibits cell growth and survival of colorectal cancer via modulating the JAK2/STAT3 signaling pathway. AZD 1480 0-7 Janus kinase 2 Homo sapiens 100-104 24953013-9 2014 The inhibition of JAK2 using JAK2-specific inhibitor AZD1480 or siRNA knockdown, in presence of AURKA overexpression, abrogated the AURKA-mediated STAT3 activation. AZD 1480 53-60 Janus kinase 2 Homo sapiens 18-22 24953013-9 2014 The inhibition of JAK2 using JAK2-specific inhibitor AZD1480 or siRNA knockdown, in presence of AURKA overexpression, abrogated the AURKA-mediated STAT3 activation. AZD 1480 53-60 Janus kinase 2 Homo sapiens 29-33 24953013-9 2014 The inhibition of JAK2 using JAK2-specific inhibitor AZD1480 or siRNA knockdown, in presence of AURKA overexpression, abrogated the AURKA-mediated STAT3 activation. AZD 1480 53-60 aurora kinase A Homo sapiens 96-101 24953013-9 2014 The inhibition of JAK2 using JAK2-specific inhibitor AZD1480 or siRNA knockdown, in presence of AURKA overexpression, abrogated the AURKA-mediated STAT3 activation. AZD 1480 53-60 aurora kinase A Homo sapiens 132-137 24953013-9 2014 The inhibition of JAK2 using JAK2-specific inhibitor AZD1480 or siRNA knockdown, in presence of AURKA overexpression, abrogated the AURKA-mediated STAT3 activation. AZD 1480 53-60 signal transducer and activator of transcription 3 Homo sapiens 147-152 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 CD34 molecule Homo sapiens 58-62 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 Janus kinase 1 Homo sapiens 81-89 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 CD34 molecule Homo sapiens 141-145 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 CD34 molecule Homo sapiens 141-145 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 Thy-1 cell surface antigen Homo sapiens 157-161 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 CD34 molecule Homo sapiens 141-145 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 Janus kinase 2 Homo sapiens 271-275 25193869-3 2014 The in vitro treatment of splenic and peripheral blood MF CD34(+) cells with the JAK1/2/3 inhibitor, AZD1480, reduced the absolute number of CD34(+), CD34(+)CD90(+), and CD34(+)CXCR4(+) cells as well as assayable hematopoietic progenitor cells (HPCs) irrespective of the JAK2 and calreticulin mutational status. AZD 1480 101-108 calreticulin Homo sapiens 280-292 25131802-0 2014 Initial solid tumor testing (stage 1) of AZD1480, an inhibitor of Janus kinases 1 and 2 by the pediatric preclinical testing program. AZD 1480 41-48 Janus kinase 1 Homo sapiens 66-87 25131802-1 2014 BACKGROUND: AZD1480 is an ATP competitive inhibitor of Janus kinases 1 and 2 (JAK1, 2) that has been shown to inhibit the growth of solid tumor models. AZD 1480 12-19 Janus kinase 1 Homo sapiens 55-76 25131802-1 2014 BACKGROUND: AZD1480 is an ATP competitive inhibitor of Janus kinases 1 and 2 (JAK1, 2) that has been shown to inhibit the growth of solid tumor models. AZD 1480 12-19 Janus kinase 1 Homo sapiens 78-82 25216185-0 2014 AZD1480, a JAK inhibitor, inhibits cell growth and survival of colorectal cancer via modulating the JAK2/STAT3 signaling pathway. AZD 1480 0-7 signal transducer and activator of transcription 3 Homo sapiens 105-110 25216185-2 2014 To develop novel therapies for CRC, we have explored the effects of a novel small-molecule JAK inhibitor (AZD1480) on IL-6/JAK/STAT3 pathway and its potential antitumor activity on the human CRC cell lines (HCT116, HT29 and SW480). AZD 1480 106-113 interleukin 6 Homo sapiens 118-122 25216185-2 2014 To develop novel therapies for CRC, we have explored the effects of a novel small-molecule JAK inhibitor (AZD1480) on IL-6/JAK/STAT3 pathway and its potential antitumor activity on the human CRC cell lines (HCT116, HT29 and SW480). AZD 1480 106-113 signal transducer and activator of transcription 3 Homo sapiens 127-132 25216185-3 2014 The results showed that, AZD1480 effectively prevents constitutive and IL-6-induced JAK2 and STAT-3 phosphorylation and exerted antitumor functional effects by a decrease in proliferation and an increase in apoptosis in CRC cells. AZD 1480 25-32 interleukin 6 Homo sapiens 71-75 25216185-3 2014 The results showed that, AZD1480 effectively prevents constitutive and IL-6-induced JAK2 and STAT-3 phosphorylation and exerted antitumor functional effects by a decrease in proliferation and an increase in apoptosis in CRC cells. AZD 1480 25-32 Janus kinase 2 Homo sapiens 84-88 25216185-3 2014 The results showed that, AZD1480 effectively prevents constitutive and IL-6-induced JAK2 and STAT-3 phosphorylation and exerted antitumor functional effects by a decrease in proliferation and an increase in apoptosis in CRC cells. AZD 1480 25-32 signal transducer and activator of transcription 3 Homo sapiens 93-99 24577942-0 2014 Pharmacologic suppression of JAK1/2 by JAK1/2 inhibitor AZD1480 potently inhibits IL-6-induced experimental prostate cancer metastases formation. AZD 1480 56-63 Janus kinase 1 Mus musculus 29-35 25149535-1 2014 AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase which inhibits STAT3 phosphorylation and tumor growth. AZD 1480 0-7 Janus kinase 1 Mus musculus 61-67 25149535-1 2014 AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase which inhibits STAT3 phosphorylation and tumor growth. AZD 1480 0-7 signal transducer and activator of transcription 3 Mus musculus 90-95 25149535-5 2014 However, AZD1480 enhanced the suppressive capacity of murine MDSCs while at the same time impairing the proliferative as well as the IFN-gamma secretion capacity of murine T cells. AZD 1480 9-16 interferon gamma Mus musculus 133-142 25149535-6 2014 The addition of AZD1480 to co-cultures of human MDSCs and T cells does not affect the suppressive activity of MDSCs but it does reduce the IFN-gamma secretion and the proliferative capacity of T cells. AZD 1480 16-23 interferon gamma Homo sapiens 139-148 24577942-0 2014 Pharmacologic suppression of JAK1/2 by JAK1/2 inhibitor AZD1480 potently inhibits IL-6-induced experimental prostate cancer metastases formation. AZD 1480 56-63 Janus kinase 1 Mus musculus 29-33 24577942-0 2014 Pharmacologic suppression of JAK1/2 by JAK1/2 inhibitor AZD1480 potently inhibits IL-6-induced experimental prostate cancer metastases formation. AZD 1480 56-63 interleukin 6 Mus musculus 82-86 24577942-8 2014 Most importantly, pharmacologic inhibition of Jak1/2 by AZD1480 suppressed IL-6-induced signaling, migratory prostate cancer cell phenotypes, and metastatic dissemination of prostate cancer in vivo in nude mice. AZD 1480 56-63 Janus kinase 1 Mus musculus 46-50 24577942-8 2014 Most importantly, pharmacologic inhibition of Jak1/2 by AZD1480 suppressed IL-6-induced signaling, migratory prostate cancer cell phenotypes, and metastatic dissemination of prostate cancer in vivo in nude mice. AZD 1480 56-63 interleukin 6 Mus musculus 75-79 24577942-9 2014 In conclusion, we demonstrate that the cytokine IL-6 directly promotes prostate cancer metastasis in vitro and in vivo via Jak-Stat3 signaling pathway, and that IL-6-driven metastasis can be effectively suppressed by pharmacologic targeting of Jak1/2 using Jak1/2 inhibitor AZD1480. AZD 1480 274-281 interleukin 6 Mus musculus 48-52 24577942-9 2014 In conclusion, we demonstrate that the cytokine IL-6 directly promotes prostate cancer metastasis in vitro and in vivo via Jak-Stat3 signaling pathway, and that IL-6-driven metastasis can be effectively suppressed by pharmacologic targeting of Jak1/2 using Jak1/2 inhibitor AZD1480. AZD 1480 274-281 interleukin 6 Mus musculus 161-165 24398427-4 2014 Here, we investigated whether the small-molecule Jak1/2 inhibitor AZD1480 confers therapeutic benefits in two mouse models of inflammation-associated gastrointestinal cancer, which are strictly dependent of excessive Stat3 activation. AZD 1480 66-73 Janus kinase 1 Mus musculus 49-55 24398427-6 2014 We find that systemic administration of AZD1480 readily replicates this effect, which is associated with reduced Stat3 activation and correlates with diminished tumor cell proliferation and increased apoptosis. AZD 1480 40-47 signal transducer and activator of transcription 3 Mus musculus 113-118 24323580-6 2014 We have used AZD1480, a JAK1/2 inhibitor, to investigate the therapeutic potential of inhibiting the JAK/STAT pathway in models of EAE. AZD 1480 13-20 Janus kinase 1 Mus musculus 24-30 24359159-2 2014 Using the C-ring fragment from our first clinical candidate AZD1480 (24), optimization of the series led to the discovery of compound 19a, a potent, orally bioavailable Jak2 inhibitor. AZD 1480 60-67 Janus kinase 2 Mus musculus 169-173 24323580-7 2014 AZD1480 treatment inhibits disease severity in myelin oligodendrocyte glycoprotein-induced classical and atypical EAE models by preventing entry of immune cells into the brain, suppressing differentiation of Th1 and Th17 cells, deactivating myeloid cells, inhibiting STAT activation in the brain, and reducing expression of proinflammatory cytokines and chemokines. AZD 1480 0-7 myelin oligodendrocyte glycoprotein Mus musculus 47-82 24323580-7 2014 AZD1480 treatment inhibits disease severity in myelin oligodendrocyte glycoprotein-induced classical and atypical EAE models by preventing entry of immune cells into the brain, suppressing differentiation of Th1 and Th17 cells, deactivating myeloid cells, inhibiting STAT activation in the brain, and reducing expression of proinflammatory cytokines and chemokines. AZD 1480 0-7 negative elongation factor complex member C/D, Th1l Mus musculus 208-211 24323580-9 2014 AZD1480 treatment was also effective in reducing ongoing paralysis induced by adoptive transfer of either pathogenic Th1 or Th17 cells. AZD 1480 0-7 negative elongation factor complex member C/D, Th1l Mus musculus 117-120 23531921-0 2013 Inhibition of STAT3 with orally active JAK inhibitor, AZD1480, decreases tumor growth in Neuroblastoma and Pediatric Sarcomas In vitro and In vivo. AZD 1480 54-61 signal transducer and activator of transcription 3 Mus musculus 14-19 24238495-3 2014 We investigated the effect of the JAK1/2 inhibitor AZD1480 on lung tumors induced by an activating EGFR mutation. AZD 1480 51-58 epidermal growth factor receptor Mus musculus 99-103 24238495-17 2014 CONCLUSION: AZD1480 may be effective against lung tumors driven by an activating EGFR mutation. AZD 1480 12-19 epidermal growth factor receptor Mus musculus 81-85 24158701-3 2013 EXPERIMENTAL DESIGN: JAK1 and JAK2 were inhibited by AZD1480 or siRNAs, and the effect of inhibition of JAK gene family on SCLC cell viability was evaluated. AZD 1480 53-60 Janus kinase 1 Homo sapiens 21-25 24158701-3 2013 EXPERIMENTAL DESIGN: JAK1 and JAK2 were inhibited by AZD1480 or siRNAs, and the effect of inhibition of JAK gene family on SCLC cell viability was evaluated. AZD 1480 53-60 Janus kinase 2 Homo sapiens 30-34 24158701-9 2013 Moreover, SCLCs underwent apoptosis after AZD1480 treatment as exemplified by the downregulation of MCL1, the accumulation of cleaved caspase 3, cleaved PARP, and increase of annexin-V-positive cells. AZD 1480 42-49 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 100-104 24158701-9 2013 Moreover, SCLCs underwent apoptosis after AZD1480 treatment as exemplified by the downregulation of MCL1, the accumulation of cleaved caspase 3, cleaved PARP, and increase of annexin-V-positive cells. AZD 1480 42-49 collagen type XI alpha 2 chain Homo sapiens 153-157 24158701-9 2013 Moreover, SCLCs underwent apoptosis after AZD1480 treatment as exemplified by the downregulation of MCL1, the accumulation of cleaved caspase 3, cleaved PARP, and increase of annexin-V-positive cells. AZD 1480 42-49 annexin A5 Homo sapiens 175-184 23531921-7 2013 AZD1480 induces cell growth inhibition and caspase-dependent apoptosis in vitro and decreases expression of STAT3 target genes, including cell cycle regulators CyclinD1, 3 and CDC25A, anti-apoptotic genes Bcl-2 and survivin, the metastasis-related factor TIMP-1 and c-Myc. AZD 1480 0-7 cell division cycle 25A Mus musculus 176-182 23531921-7 2013 AZD1480 induces cell growth inhibition and caspase-dependent apoptosis in vitro and decreases expression of STAT3 target genes, including cell cycle regulators CyclinD1, 3 and CDC25A, anti-apoptotic genes Bcl-2 and survivin, the metastasis-related factor TIMP-1 and c-Myc. AZD 1480 0-7 B cell leukemia/lymphoma 2 Mus musculus 205-210 23942095-0 2013 Pharmacologic inhibition of Jak2-Stat5 signaling By Jak2 inhibitor AZD1480 potently suppresses growth of both primary and castrate-resistant prostate cancer. AZD 1480 67-74 Janus kinase 2 Mus musculus 28-32 23942095-0 2013 Pharmacologic inhibition of Jak2-Stat5 signaling By Jak2 inhibitor AZD1480 potently suppresses growth of both primary and castrate-resistant prostate cancer. AZD 1480 67-74 signal transducer and activator of transcription 5A Mus musculus 33-38 23942095-0 2013 Pharmacologic inhibition of Jak2-Stat5 signaling By Jak2 inhibitor AZD1480 potently suppresses growth of both primary and castrate-resistant prostate cancer. AZD 1480 67-74 Janus kinase 2 Mus musculus 52-56 23942095-3 2013 Here, we show that pharmacologic targeting of Jak2-dependent Stat5a/b signaling by the Jak2 inhibitor AZD1480 blocks castrate-resistant growth of prostate cancer. AZD 1480 102-109 Janus kinase 2 Mus musculus 46-50 23942095-3 2013 Here, we show that pharmacologic targeting of Jak2-dependent Stat5a/b signaling by the Jak2 inhibitor AZD1480 blocks castrate-resistant growth of prostate cancer. AZD 1480 102-109 signal transducer and activator of transcription 5A Mus musculus 61-67 23942095-3 2013 Here, we show that pharmacologic targeting of Jak2-dependent Stat5a/b signaling by the Jak2 inhibitor AZD1480 blocks castrate-resistant growth of prostate cancer. AZD 1480 102-109 Janus kinase 2 Mus musculus 87-91 23942095-4 2013 EXPERIMENTAL DESIGN: Efficacy of AZD1480 in disrupting Jak2-Stat5a/b signaling and decreasing prostate cancer cell viability was evaluated in prostate cancer cells. AZD 1480 33-40 Janus kinase 2 Mus musculus 55-59 23942095-4 2013 EXPERIMENTAL DESIGN: Efficacy of AZD1480 in disrupting Jak2-Stat5a/b signaling and decreasing prostate cancer cell viability was evaluated in prostate cancer cells. AZD 1480 33-40 signal transducer and activator of transcription 5A Mus musculus 60-66 23942095-7 2013 RESULTS: AZD1480 robustly inhibited Stat5a/b phosphorylation, dimerization, nuclear translocation, DNA binding, and transcriptional activity in prostate cancer cells. AZD 1480 9-16 signal transducer and activator of transcription 5A Mus musculus 36-42 23942095-8 2013 AZD1480 reduced prostate cancer cell viability sustained by Jak2-Stat5a/b signaling through induction of apoptosis, which was rescued by constitutively active Stat5a/b. AZD 1480 0-7 Janus kinase 2 Mus musculus 60-64 23942095-8 2013 AZD1480 reduced prostate cancer cell viability sustained by Jak2-Stat5a/b signaling through induction of apoptosis, which was rescued by constitutively active Stat5a/b. AZD 1480 0-7 signal transducer and activator of transcription 5A Mus musculus 65-71 23942095-8 2013 AZD1480 reduced prostate cancer cell viability sustained by Jak2-Stat5a/b signaling through induction of apoptosis, which was rescued by constitutively active Stat5a/b. AZD 1480 0-7 signal transducer and activator of transcription 5A Mus musculus 159-165 23942095-9 2013 In mice, pharmacologic targeting of Stat5a/b by AZD1480 potently blocked growth of primary androgen-dependent as well as recurrent castrate-resistant CWR22Pc xenograft tumors, and prolonged survival of tumor-bearing mice versus vehicle or docetaxel-treated mice. AZD 1480 48-55 signal transducer and activator of transcription 5A Mus musculus 36-42 23942095-10 2013 Finally, nine of 12 clinical prostate cancers responded to AZD1480 by extensive apoptotic epithelial cell loss, concurrent with reduced levels of nuclear Stat5a/b. AZD 1480 59-66 signal transducer and activator of transcription 5A Mus musculus 154-160 23531921-7 2013 AZD1480 induces cell growth inhibition and caspase-dependent apoptosis in vitro and decreases expression of STAT3 target genes, including cell cycle regulators CyclinD1, 3 and CDC25A, anti-apoptotic genes Bcl-2 and survivin, the metastasis-related factor TIMP-1 and c-Myc. AZD 1480 0-7 baculoviral IAP repeat-containing 5 Mus musculus 215-223 23531921-7 2013 AZD1480 induces cell growth inhibition and caspase-dependent apoptosis in vitro and decreases expression of STAT3 target genes, including cell cycle regulators CyclinD1, 3 and CDC25A, anti-apoptotic genes Bcl-2 and survivin, the metastasis-related factor TIMP-1 and c-Myc. AZD 1480 0-7 tissue inhibitor of metalloproteinase 1 Mus musculus 255-261 23531921-9 2013 Tumors from AZD1480-treated mice showed inhibition of activated STAT3 as well as decreased expression of STAT3 downstream targets. AZD 1480 12-19 signal transducer and activator of transcription 3 Mus musculus 64-69 23531921-9 2013 Tumors from AZD1480-treated mice showed inhibition of activated STAT3 as well as decreased expression of STAT3 downstream targets. AZD 1480 12-19 signal transducer and activator of transcription 3 Mus musculus 105-110 23531921-10 2013 Our study provides strong evidence of the anti-tumor growth potency of JAK inhibitor AZD1480 in pediatric solid tumors, providing proof-of principle that inhibition of the JAK/STAT3 signal transduction could be a promising therapeutic target for high-risk pediatric solid tumors. AZD 1480 85-92 signal transducer and activator of transcription 3 Mus musculus 176-181 23531921-2 2013 AZD1480, a pharmacological JAK1/2 inhibitor, exhibits anti-tumor potency in multiple adult malignancies. AZD 1480 0-7 Janus kinase 1 Mus musculus 27-33 23531921-5 2013 Our data indicate that AZD1480 blocks endogenous as well as IL-6 induced STAT3 activation. AZD 1480 23-30 interleukin 6 Mus musculus 60-64 23531921-5 2013 Our data indicate that AZD1480 blocks endogenous as well as IL-6 induced STAT3 activation. AZD 1480 23-30 signal transducer and activator of transcription 3 Mus musculus 73-78 23531921-7 2013 AZD1480 induces cell growth inhibition and caspase-dependent apoptosis in vitro and decreases expression of STAT3 target genes, including cell cycle regulators CyclinD1, 3 and CDC25A, anti-apoptotic genes Bcl-2 and survivin, the metastasis-related factor TIMP-1 and c-Myc. AZD 1480 0-7 signal transducer and activator of transcription 3 Mus musculus 108-113 23847256-0 2013 AZD1480: a phase I study of a novel JAK2 inhibitor in solid tumors. AZD 1480 0-7 Janus kinase 2 Homo sapiens 36-40 24083752-4 2013 After treatment with AZD1480 plus cisplatin, the apoptosis rate increased significantly while the expression level of p-STAT3 protein was decreased. AZD 1480 21-28 signal transducer and activator of transcription 3 Homo sapiens 120-125 24083752-5 2013 CONCLUSION: AZD1480 can inhibit the proliferation, invasion, metastasis and clone formation of SKOV3 cells, induce cellulsar apoptosis, increase the chemotherapeutic sensitivity and reduce the expression level of p-STAT3 protein. AZD 1480 12-19 signal transducer and activator of transcription 3 Homo sapiens 215-220 23847256-1 2013 BACKGROUND: AZD1480 is a novel agent that inhibits Janus-associated kinases 1 and 2 (JAK1 and JAK2). AZD 1480 12-19 Janus kinase 1 Homo sapiens 85-89 23847256-1 2013 BACKGROUND: AZD1480 is a novel agent that inhibits Janus-associated kinases 1 and 2 (JAK1 and JAK2). AZD 1480 12-19 Janus kinase 2 Homo sapiens 94-98 22355274-0 2012 Comparisons of the efficacy of a Jak1/2 inhibitor (AZD1480) with a VEGF signaling inhibitor (cediranib) and sham treatments in mouse tumors using DCE-MRI, DW-MRI, and histology. AZD 1480 51-58 Janus kinase 1 Mus musculus 33-39 23013619-4 2012 Administration of the JAK/STAT3 inhibitor AZD1480 alone and in combination with cediranib reduced tumor hypoxia and the infiltration of VEGF inhibitor-induced p-STAT3 macrophages. AZD 1480 42-49 signal transducer and activator of transcription 3 Homo sapiens 26-31 23013619-4 2012 Administration of the JAK/STAT3 inhibitor AZD1480 alone and in combination with cediranib reduced tumor hypoxia and the infiltration of VEGF inhibitor-induced p-STAT3 macrophages. AZD 1480 42-49 vascular endothelial growth factor A Homo sapiens 136-140 23013619-4 2012 Administration of the JAK/STAT3 inhibitor AZD1480 alone and in combination with cediranib reduced tumor hypoxia and the infiltration of VEGF inhibitor-induced p-STAT3 macrophages. AZD 1480 42-49 signal transducer and activator of transcription 3 Homo sapiens 161-166 23013619-5 2012 Thus, the combination of AZD1480 with cediranib markedly reduced tumor volume, and microvascular density, indicating that up regulation of the STAT3 pathway can mediate resistance to antiangiogenic therapy and combinational approaches may delay or overcome resistance. AZD 1480 25-32 signal transducer and activator of transcription 3 Homo sapiens 143-148 21926964-7 2012 Our results further indicated that these mutations also conferred cross-resistance to all JAK2 kinase inhibitors tested, including AZD1480, TG101348, lestaurtinib (CEP-701) and CYT-387. AZD 1480 131-138 Janus kinase 2 Mus musculus 90-94 22355274-3 2012 AZD1480 is a novel small molecule inhibitor of Jak1/2, which is a key mediator of STAT3 activation. AZD 1480 0-7 Janus kinase 1 Mus musculus 47-53 22355274-3 2012 AZD1480 is a novel small molecule inhibitor of Jak1/2, which is a key mediator of STAT3 activation. AZD 1480 0-7 signal transducer and activator of transcription 3 Mus musculus 82-87 23056499-0 2012 AZD1480 blocks growth and tumorigenesis of RET- activated thyroid cancer cell lines. AZD 1480 0-7 ret proto-oncogene Homo sapiens 43-46 23056499-3 2012 Here, we tested the efficacy of a JAK1/2- inhibitor, AZD1480, in the in vitro and in vivo growth of thyroid cancer cell lines expressing oncogenic RET. AZD 1480 53-60 Janus kinase 1 Homo sapiens 34-38 23056499-3 2012 Here, we tested the efficacy of a JAK1/2- inhibitor, AZD1480, in the in vitro and in vivo growth of thyroid cancer cell lines expressing oncogenic RET. AZD 1480 53-60 ret proto-oncogene Homo sapiens 147-150 23056499-7 2012 However, AZD1480 repressed the growth of STAT3- deficient TPC-1 cells in vitro and in vivo, demonstrating that its effects in this cell line were independent of STAT3 in the tumor cells. AZD 1480 9-16 signal transducer and activator of transcription 3 Homo sapiens 41-46 23056499-7 2012 However, AZD1480 repressed the growth of STAT3- deficient TPC-1 cells in vitro and in vivo, demonstrating that its effects in this cell line were independent of STAT3 in the tumor cells. AZD 1480 9-16 two pore segment channel 1 Homo sapiens 58-63 23056499-9 2012 In conclusion, AZD1480 effectively blocks proliferation and tumor growth of activated RET- thyroid cancer cell lines, likely through direct RET inhibition in cancer cells as well as by modulation of the microenvironment (e.g. via JAK/phospho-STAT3 inhibition in endothelial cells). AZD 1480 15-22 ret proto-oncogene Homo sapiens 86-89 23056499-9 2012 In conclusion, AZD1480 effectively blocks proliferation and tumor growth of activated RET- thyroid cancer cell lines, likely through direct RET inhibition in cancer cells as well as by modulation of the microenvironment (e.g. via JAK/phospho-STAT3 inhibition in endothelial cells). AZD 1480 15-22 ret proto-oncogene Homo sapiens 140-143 23056499-9 2012 In conclusion, AZD1480 effectively blocks proliferation and tumor growth of activated RET- thyroid cancer cell lines, likely through direct RET inhibition in cancer cells as well as by modulation of the microenvironment (e.g. via JAK/phospho-STAT3 inhibition in endothelial cells). AZD 1480 15-22 signal transducer and activator of transcription 3 Homo sapiens 242-247 23056499-10 2012 Thus, AZD1480 should be considered as a therapeutic agent for the treatment of RET- activated thyroid cancers. AZD 1480 6-13 ret proto-oncogene Homo sapiens 79-82 22829094-3 2011 AZD1480 at low doses (0.1-1 mu) potently inhibited STATs phosphorylation, but did not predictably result in antiproliferative effects, as it activated a negative-feedback loop causing phosphorylation of JAK2 and extracellular signal-regulated kinases 1 and 2 (ERK1/2), and increased IP-10, RANTES and interleukin (IL)-8 concentrations in the supernatants. AZD 1480 0-7 Janus kinase 2 Homo sapiens 203-207 22829094-3 2011 AZD1480 at low doses (0.1-1 mu) potently inhibited STATs phosphorylation, but did not predictably result in antiproliferative effects, as it activated a negative-feedback loop causing phosphorylation of JAK2 and extracellular signal-regulated kinases 1 and 2 (ERK1/2), and increased IP-10, RANTES and interleukin (IL)-8 concentrations in the supernatants. AZD 1480 0-7 mitogen-activated protein kinase 1 Homo sapiens 212-258 22829094-3 2011 AZD1480 at low doses (0.1-1 mu) potently inhibited STATs phosphorylation, but did not predictably result in antiproliferative effects, as it activated a negative-feedback loop causing phosphorylation of JAK2 and extracellular signal-regulated kinases 1 and 2 (ERK1/2), and increased IP-10, RANTES and interleukin (IL)-8 concentrations in the supernatants. AZD 1480 0-7 mitogen-activated protein kinase 3 Homo sapiens 260-266 22829094-3 2011 AZD1480 at low doses (0.1-1 mu) potently inhibited STATs phosphorylation, but did not predictably result in antiproliferative effects, as it activated a negative-feedback loop causing phosphorylation of JAK2 and extracellular signal-regulated kinases 1 and 2 (ERK1/2), and increased IP-10, RANTES and interleukin (IL)-8 concentrations in the supernatants. AZD 1480 0-7 C-X-C motif chemokine ligand 10 Homo sapiens 283-288 22829094-3 2011 AZD1480 at low doses (0.1-1 mu) potently inhibited STATs phosphorylation, but did not predictably result in antiproliferative effects, as it activated a negative-feedback loop causing phosphorylation of JAK2 and extracellular signal-regulated kinases 1 and 2 (ERK1/2), and increased IP-10, RANTES and interleukin (IL)-8 concentrations in the supernatants. AZD 1480 0-7 C-C motif chemokine ligand 5 Homo sapiens 290-296 22829094-3 2011 AZD1480 at low doses (0.1-1 mu) potently inhibited STATs phosphorylation, but did not predictably result in antiproliferative effects, as it activated a negative-feedback loop causing phosphorylation of JAK2 and extracellular signal-regulated kinases 1 and 2 (ERK1/2), and increased IP-10, RANTES and interleukin (IL)-8 concentrations in the supernatants. AZD 1480 0-7 C-X-C motif chemokine ligand 8 Homo sapiens 301-319 22829094-4 2011 Inhibition of the ERK activity by mitogen-activated extracellular signal regulated kinase (MEK) inhibitors (UO126 and PD98059) enhanced the cytotoxic activity of AZD1480. AZD 1480 162-169 mitogen-activated protein kinase 3 Homo sapiens 18-21 22829094-4 2011 Inhibition of the ERK activity by mitogen-activated extracellular signal regulated kinase (MEK) inhibitors (UO126 and PD98059) enhanced the cytotoxic activity of AZD1480. AZD 1480 162-169 mitogen-activated protein kinase kinase 7 Homo sapiens 91-94 22829094-5 2011 Interestingly, submicromolar concentrations of AZD1480 demonstrated significant immunoregulatory effects by downregulating T-helper 2 cytokines and chemokines, including IL-13 and thymus- and activation-regulated chemokine, and the surface expression of the immunosuppressive programmed death ligands 1 and 2. AZD 1480 47-54 interleukin 13 Homo sapiens 170-222 22027691-4 2011 AZD1480 treatment effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. AZD 1480 0-7 Janus kinase 1 Homo sapiens 71-75 22027691-4 2011 AZD1480 treatment effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. AZD 1480 0-7 Janus kinase 2 Homo sapiens 77-81 22027691-4 2011 AZD1480 treatment effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. AZD 1480 0-7 signal transducer and activator of transcription 3 Homo sapiens 87-93 22027691-7 2011 AZD1480 inhibits constitutive and stimulus-induced phosphorylation of JAK2 and STAT-3 in these GBM xenograft tumors in vitro, downstream gene expression, and inhibits cell proliferation. AZD 1480 0-7 Janus kinase 2 Homo sapiens 70-74 22027691-7 2011 AZD1480 inhibits constitutive and stimulus-induced phosphorylation of JAK2 and STAT-3 in these GBM xenograft tumors in vitro, downstream gene expression, and inhibits cell proliferation. AZD 1480 0-7 signal transducer and activator of transcription 3 Homo sapiens 79-85 22027691-8 2011 Furthermore, AZD1480 suppresses STAT-3 activation in the glioma-initiating cell population in GBM tumors. AZD 1480 13-20 signal transducer and activator of transcription 3 Homo sapiens 32-38 22027691-9 2011 In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial GBM tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. AZD 1480 9-16 signal transducer and activator of transcription 3 Mus musculus 137-143 22027691-9 2011 In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial GBM tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. AZD 1480 9-16 signal transducer and activator of transcription 3 Mus musculus 206-212 21164517-0 2011 The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival. AZD 1480 24-31 signal transducer and activator of transcription 3 Homo sapiens 39-44 21164517-0 2011 The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival. AZD 1480 24-31 fibroblast growth factor receptor 3 Homo sapiens 49-54 21164517-2 2011 We investigated the effects of a novel small-molecule JAK inhibitor (AZD1480) on IL-6/JAK signal transduction and its biological consequences on the human myeloma-derived cell lines U266 and Kms.11. AZD 1480 69-76 interleukin 6 Homo sapiens 81-85 21164517-4 2011 These biological responses to AZD1480 are associated with concomitant inhibition of phosphorylation of JAK2, STAT3 and MAPK signaling proteins. AZD 1480 30-37 Janus kinase 2 Homo sapiens 103-107 21164517-4 2011 These biological responses to AZD1480 are associated with concomitant inhibition of phosphorylation of JAK2, STAT3 and MAPK signaling proteins. AZD 1480 30-37 signal transducer and activator of transcription 3 Homo sapiens 109-114 21164517-6 2011 Examination of a wider variety of myeloma cells (RPMI 8226, OPM-2, NCI-H929, Kms.18, MM1.S and IM-9), as well as primary myeloma cells, showed that AZD1480 has broad efficacy. AZD 1480 148-155 plexin B2 Homo sapiens 85-88 21164517-8 2011 Importantly, AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD 1480 13-20 fibroblast growth factor receptor 3 Mus musculus 225-230 21164517-8 2011 Importantly, AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD 1480 13-20 Janus kinase 2 Mus musculus 240-244 21164517-8 2011 Importantly, AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD 1480 13-20 signal transducer and activator of transcription 3 Mus musculus 254-259 21164517-8 2011 Importantly, AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD 1480 13-20 cyclin D2 Mus musculus 264-273 21164517-9 2011 In sum, AZD1480 blocks proliferation, survival, FGFR3 and JAK/STAT3 signaling in myeloma cells cultured alone or cocultured with BM stromal cells, and in vivo. AZD 1480 8-15 fibroblast growth factor receptor 3 Homo sapiens 48-53 21164517-9 2011 In sum, AZD1480 blocks proliferation, survival, FGFR3 and JAK/STAT3 signaling in myeloma cells cultured alone or cocultured with BM stromal cells, and in vivo. AZD 1480 8-15 signal transducer and activator of transcription 3 Homo sapiens 62-67 21138246-3 2011 Herein, we disclose the discovery of a series of pyrazol-3-yl pyrimidin-4-amines and the identification of 9e (AZD1480) as a potent Jak2 inhibitor. AZD 1480 111-118 Janus kinase 2 Homo sapiens 132-136 19962667-0 2009 The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. AZD 1480 19-26 Janus kinase 2 Homo sapiens 4-8 19962667-0 2009 The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. AZD 1480 19-26 signal transducer and activator of transcription 3 Homo sapiens 43-48 19962667-5 2009 The Jak2 inhibitor AZD1480 suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity. AZD 1480 19-26 Janus kinase 2 Homo sapiens 4-8 19962667-5 2009 The Jak2 inhibitor AZD1480 suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity. AZD 1480 19-26 signal transducer and activator of transcription 3 Homo sapiens 102-107 21920898-4 2011 In this study, we show that AZD1480 inhibits STAT3 in tumor-associated myeloid cells, reducing their number and inhibiting tumor metastasis. AZD 1480 28-35 signal transducer and activator of transcription 3 Homo sapiens 45-50 21920898-9 2011 Together, our results indicated that AZD1480 can effectively inhibit tumor angiogenesis and metastasis mediated by STAT3 in stromal cells as well as tumor cells. AZD 1480 37-44 signal transducer and activator of transcription 3 Homo sapiens 115-120 21751940-4 2011 We also review the rationale to use novel STAT3 inhibitors and list some of these inhibitors such as STA-21, IS3 295, S3I- M2001 and small molecule JAK2 inhibitors AZD1480 and AZ960 that have been found to be efficient against tumors. AZD 1480 164-171 signal transducer and activator of transcription 3 Homo sapiens 42-47 21751940-4 2011 We also review the rationale to use novel STAT3 inhibitors and list some of these inhibitors such as STA-21, IS3 295, S3I- M2001 and small molecule JAK2 inhibitors AZD1480 and AZ960 that have been found to be efficient against tumors. AZD 1480 164-171 Janus kinase 2 Homo sapiens 148-152