PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 28983639-3 2019 Cells treated with the Pyk2 inhibitor TAE226 and PI3K inhibitor LY294002 were used for additional experiments. TAE226 38-44 protein tyrosine kinase 2 beta Homo sapiens 23-27 34784956-0 2021 Focal adhesion kinase inhibitor TAE226 combined with Sorafenib slows down hepatocellular carcinoma by multiple epigenetic effects. TAE226 32-38 PTK2 protein tyrosine kinase 2 Mus musculus 0-21 34784956-9 2021 Combined TAE226 and SOR treatment reduced HCC growth both in vitro and in vivo by affecting tumour-promoting gene expression and inducing epigenetic changes via dysregulation of FAK nuclear interactome. TAE226 9-15 PTK2 protein tyrosine kinase 2 Mus musculus 178-181 34784956-11 2021 TAE226-mediated FAK depletion and SOR-promoted MAPK down-modulation caused a decrease in the nuclear amount of HDAC1/2 and a consequent increase of the histone H3 lysine 27 acetylation, thus counteracting histone H3 lysine 27 trimethylation. TAE226 0-6 PTK2 protein tyrosine kinase 2 Mus musculus 16-19 34784956-11 2021 TAE226-mediated FAK depletion and SOR-promoted MAPK down-modulation caused a decrease in the nuclear amount of HDAC1/2 and a consequent increase of the histone H3 lysine 27 acetylation, thus counteracting histone H3 lysine 27 trimethylation. TAE226 0-6 histone deacetylase 1 Mus musculus 111-118 32979460-6 2020 An inhibitor of focal adhesion kinase (FAK) phosphorylation, TAE226, was used to demonstrate a relationship between extracellular adhesion perturbations and structural reactivity in the novel 3D model. TAE226 61-67 protein tyrosine kinase 2 Homo sapiens 16-37 32979460-6 2020 An inhibitor of focal adhesion kinase (FAK) phosphorylation, TAE226, was used to demonstrate a relationship between extracellular adhesion perturbations and structural reactivity in the novel 3D model. TAE226 61-67 protein tyrosine kinase 2 Homo sapiens 39-42 34757216-1 2021 Forty-one new focal adhesion kinase (FAK) covalent inhibitors were designed and synthesized based on FAK inhibitor TAE226. TAE226 115-121 protein tyrosine kinase 2 Homo sapiens 14-35 34757216-1 2021 Forty-one new focal adhesion kinase (FAK) covalent inhibitors were designed and synthesized based on FAK inhibitor TAE226. TAE226 115-121 protein tyrosine kinase 2 Homo sapiens 37-40 34757216-1 2021 Forty-one new focal adhesion kinase (FAK) covalent inhibitors were designed and synthesized based on FAK inhibitor TAE226. TAE226 115-121 protein tyrosine kinase 2 Homo sapiens 101-104 35452915-0 2022 Design, synthesis and biological evaluation of novel FAK inhibitors with better selectivity over IR than TAE226. TAE226 105-111 protein tyrosine kinase 2 Homo sapiens 53-56 35452915-1 2022 In this study, 28 novel focal adhesion kinase (FAK) inhibitors were designed and synthesized based on FAK inhibitor TAE226. TAE226 116-122 protein tyrosine kinase 2 Homo sapiens 24-45 35452915-1 2022 In this study, 28 novel focal adhesion kinase (FAK) inhibitors were designed and synthesized based on FAK inhibitor TAE226. TAE226 116-122 protein tyrosine kinase 2 Homo sapiens 47-50 35452915-1 2022 In this study, 28 novel focal adhesion kinase (FAK) inhibitors were designed and synthesized based on FAK inhibitor TAE226. TAE226 116-122 protein tyrosine kinase 2 Homo sapiens 102-105 32784087-5 2020 Furthermore, computational docking analysis also suggested that 4o and TAE-226 displayed the similar interaction with FAK kinase domain. TAE226 71-78 protein tyrosine kinase 2 Homo sapiens 118-121 31215459-0 2019 Pharmacological profiling of a dual FAK/IGF-1R kinase inhibitor TAE226 in cellular and in vivo tumor models. TAE226 64-70 PTK2 protein tyrosine kinase 2 Mus musculus 36-39 31215459-0 2019 Pharmacological profiling of a dual FAK/IGF-1R kinase inhibitor TAE226 in cellular and in vivo tumor models. TAE226 64-70 insulin-like growth factor I receptor Mus musculus 40-46 31215459-1 2019 OBJECTIVE: A dual inhibitor of focal adhesion kinase (FAK) and insulin-like growth factor 1 receptor (IGF-1R), TAE226, was evaluated in a panel of cancer cell lines, MIA PaCa-2 human pancreatic tumor and 4T1 murine breast tumor models. TAE226 111-117 insulin like growth factor 1 receptor Homo sapiens 63-100 31215459-1 2019 OBJECTIVE: A dual inhibitor of focal adhesion kinase (FAK) and insulin-like growth factor 1 receptor (IGF-1R), TAE226, was evaluated in a panel of cancer cell lines, MIA PaCa-2 human pancreatic tumor and 4T1 murine breast tumor models. TAE226 111-117 insulin like growth factor 1 receptor Homo sapiens 102-108 31215459-7 2019 In the MIA PaCa-2 model, TAE226 inhibited phosphorylation of Y397-FAK and phosphorylation of S473-Akt as IGF-1R signaling in the cell culture in vitro and the tumor in mice. TAE226 25-31 PTK2 protein tyrosine kinase 2 Mus musculus 66-69 31215459-7 2019 In the MIA PaCa-2 model, TAE226 inhibited phosphorylation of Y397-FAK and phosphorylation of S473-Akt as IGF-1R signaling in the cell culture in vitro and the tumor in mice. TAE226 25-31 thymoma viral proto-oncogene 1 Mus musculus 98-101 31215459-7 2019 In the MIA PaCa-2 model, TAE226 inhibited phosphorylation of Y397-FAK and phosphorylation of S473-Akt as IGF-1R signaling in the cell culture in vitro and the tumor in mice. TAE226 25-31 insulin-like growth factor I receptor Mus musculus 105-111 31215459-9 2019 Similarly in the 4T1 model, TAE226 inhibited phosphorylation of Y397-FAK and S473-Akt in the cell culture in vitro and the tumor in mice. TAE226 28-34 PTK2 protein tyrosine kinase 2 Mus musculus 69-72 31215459-9 2019 Similarly in the 4T1 model, TAE226 inhibited phosphorylation of Y397-FAK and S473-Akt in the cell culture in vitro and the tumor in mice. TAE226 28-34 thymoma viral proto-oncogene 1 Mus musculus 82-85 30228782-9 2018 The results of TAE226, U0126 or Ly294002 treatment confirmed an essential role of FMNL3 in activation of the RhoC/FAK pathway and the subsequent promotion of CRC invasion. TAE226 15-21 formin like 3 Homo sapiens 82-87 26096850-4 2015 beta1 integrin, focal adhesion kinase and EGFR were inhibited by AIIB2, TAE226 and Cetuximab, respectively. TAE226 72-78 integrin subunit beta 1 Homo sapiens 0-14 29458087-7 2018 However, the tissue scores was signifcaintly decreased by FAK inhibitor TAE226. TAE226 72-78 protein tyrosine kinase 2 Rattus norvegicus 58-61 27704688-4 2017 These abnormalities were ameliorated by dietary intervention of TAE226, a reported inhibitor of FAK. TAE226 64-70 protein tyrosine kinase 2 Rattus norvegicus 96-99 27704688-9 2017 This was further identified by animal data that p38 activation was also abrogated by TAE226 treatment in hypercholesterolaemic rats, suggesting that FAK/p38 axis might also be involved in in vivo events. TAE226 85-91 mitogen activated protein kinase 14 Rattus norvegicus 48-51 27704688-9 2017 This was further identified by animal data that p38 activation was also abrogated by TAE226 treatment in hypercholesterolaemic rats, suggesting that FAK/p38 axis might also be involved in in vivo events. TAE226 85-91 protein tyrosine kinase 2 Rattus norvegicus 149-152 27704688-9 2017 This was further identified by animal data that p38 activation was also abrogated by TAE226 treatment in hypercholesterolaemic rats, suggesting that FAK/p38 axis might also be involved in in vivo events. TAE226 85-91 mitogen activated protein kinase 14 Rattus norvegicus 153-156 26549408-4 2016 In the present article, we used Molecular Dynamic (MD) simulation method to explore the characteristic of interaction between FAK and three inhibitors (PHM16, TAE226, and ligand3). TAE226 159-165 protein tyrosine kinase 2 Homo sapiens 126-129 29090460-3 2017 When we treated RAW 264.7 macrophages with inhibitors of various oncogenic pathways, we found that the focal adhesion kinase (FAK) inhibitors PF573228 and TAE226 could induce cell multinucleation by suppressing furrowing and cytokinesis. TAE226 155-161 PTK2 protein tyrosine kinase 2 Mus musculus 103-124 29090460-3 2017 When we treated RAW 264.7 macrophages with inhibitors of various oncogenic pathways, we found that the focal adhesion kinase (FAK) inhibitors PF573228 and TAE226 could induce cell multinucleation by suppressing furrowing and cytokinesis. TAE226 155-161 PTK2 protein tyrosine kinase 2 Mus musculus 126-129 27380318-5 2016 Treatment of goat fetal fibroblasts (GFbs) with a specific FAK inhibitor, TAE226, inhibited cell proliferation (p < 0.05) and induced damage to the cell morphology in a dose- and time-dependent manner. TAE226 74-80 focal adhesion kinase 1 Capra hircus 59-62 27531475-0 2016 [Therapeutic effect of IGF-1R-targeting inhibitor (TAE226) on malignant pleural effusion in nude mice]. TAE226 51-57 insulin-like growth factor I receptor Mus musculus 23-29 27531475-1 2016 OBJECTIVE: To study the therapeutic effect of IGF-1R inhibitor TAE226 on malignant pleural effusion (MPE) in nude mice. TAE226 63-69 insulin-like growth factor I receptor Mus musculus 46-52 26096850-4 2015 beta1 integrin, focal adhesion kinase and EGFR were inhibited by AIIB2, TAE226 and Cetuximab, respectively. TAE226 72-78 epidermal growth factor receptor Homo sapiens 42-46 24915008-6 2014 Treatment of Alport mice with TAE226, a small molecule inhibitor of FAK activation, ameliorated fibrosis and glomerulosclerosis, significantly reduced proteinuria and blood urea nitrogen levels, and partially restored GBM ultrastructure. TAE226 30-36 PTK2 protein tyrosine kinase 2 Mus musculus 68-71 25625667-3 2015 Thus, FAK was inhibited using the pharmaco-logical inhibitor TAE226 and cytotoxicity and radiosensitization of glioblastoma cells were investigated in vitro. TAE226 61-67 protein tyrosine kinase 2 Homo sapiens 6-9 25625667-6 2015 Efficient FAK inhibition by TAE226 mediated significant cytotoxicity and reduced sphere formation in a dose- and time-dependent manner. TAE226 28-34 protein tyrosine kinase 2 Homo sapiens 10-13 25625667-9 2015 The results demonstrated that pharmacological FAK inhibitor TAE226 efficiently reduced clonogenicity and sphere formation in glioblastoma cells without generally modifying their radiosensitivity. TAE226 60-66 protein tyrosine kinase 2 Homo sapiens 46-49 25625667-10 2015 However, future studies are necessary to define the potential of FAK inhibition by TAE226 or other pharmacological inhibitors in combination with radiochemotherapy. TAE226 83-89 protein tyrosine kinase 2 Homo sapiens 65-68 26090892-0 2015 TAE226, a Bis-Anilino Pyrimidine Compound, Inhibits the EGFR-Mutant Kinase Including T790M Mutant to Show Anti-Tumor Effect on EGFR-Mutant Non-Small Cell Lung Cancer Cells. TAE226 0-6 epidermal growth factor receptor Mus musculus 56-60 26090892-0 2015 TAE226, a Bis-Anilino Pyrimidine Compound, Inhibits the EGFR-Mutant Kinase Including T790M Mutant to Show Anti-Tumor Effect on EGFR-Mutant Non-Small Cell Lung Cancer Cells. TAE226 0-6 epidermal growth factor receptor Mus musculus 127-131 26090892-1 2015 TAE226, a bis-anilino pyrimidine compound, has been developed as an inhibitor of focal adhesion kinase (FAK) and insulin-like growth factor-I receptor (IGF-IR). TAE226 0-6 PTK2 protein tyrosine kinase 2 Mus musculus 81-102 26090892-1 2015 TAE226, a bis-anilino pyrimidine compound, has been developed as an inhibitor of focal adhesion kinase (FAK) and insulin-like growth factor-I receptor (IGF-IR). TAE226 0-6 PTK2 protein tyrosine kinase 2 Mus musculus 104-107 26090892-1 2015 TAE226, a bis-anilino pyrimidine compound, has been developed as an inhibitor of focal adhesion kinase (FAK) and insulin-like growth factor-I receptor (IGF-IR). TAE226 0-6 insulin-like growth factor I receptor Mus musculus 113-150 26090892-1 2015 TAE226, a bis-anilino pyrimidine compound, has been developed as an inhibitor of focal adhesion kinase (FAK) and insulin-like growth factor-I receptor (IGF-IR). TAE226 0-6 insulin-like growth factor I receptor Mus musculus 152-158 26090892-3 2015 TAE226 was more effective against cells with mutant EGFR, including the T790M mutant, than against cells with wild-type one. TAE226 0-6 epidermal growth factor receptor Mus musculus 52-56 26090892-4 2015 TAE226 preferentially inhibited phospho-EGFR and its downstream signaling mediators in the cells with mutant EGFR than in those with wild-type one. TAE226 0-6 epidermal growth factor receptor Mus musculus 40-44 26090892-4 2015 TAE226 preferentially inhibited phospho-EGFR and its downstream signaling mediators in the cells with mutant EGFR than in those with wild-type one. TAE226 0-6 epidermal growth factor receptor Mus musculus 109-113 26090892-7 2015 Of interest, the L858R/T790M or delE746_A750/T790M mutant enhanced the binding affinity for TAE226 compared with the L858R or delE746_A750 mutant, resulting in the effectiveness of TAE226 against T790M mutant cells despite the T790M mutation restoring the ATP affinity for the mutant EGFR close to that for the wild-type. TAE226 92-98 epidermal growth factor receptor Mus musculus 284-288 26090892-7 2015 Of interest, the L858R/T790M or delE746_A750/T790M mutant enhanced the binding affinity for TAE226 compared with the L858R or delE746_A750 mutant, resulting in the effectiveness of TAE226 against T790M mutant cells despite the T790M mutation restoring the ATP affinity for the mutant EGFR close to that for the wild-type. TAE226 181-187 epidermal growth factor receptor Mus musculus 284-288 26090892-10 2015 In summary, we showed that TAE226 inhibited the activation of mutant EGFR and exhibited anti-proliferative activity against NSCLCs carrying EGFR mutations, including T790M mutation. TAE226 27-33 epidermal growth factor receptor Mus musculus 69-73 26090892-10 2015 In summary, we showed that TAE226 inhibited the activation of mutant EGFR and exhibited anti-proliferative activity against NSCLCs carrying EGFR mutations, including T790M mutation. TAE226 27-33 epidermal growth factor receptor Mus musculus 140-144 24915008-7 2014 Glomerular expression of MMP-9, MMP-10 and MMP-12 mRNAs was significantly reduced in TAE226 treated animals. TAE226 85-91 matrix metallopeptidase 9 Mus musculus 25-30 24915008-7 2014 Glomerular expression of MMP-9, MMP-10 and MMP-12 mRNAs was significantly reduced in TAE226 treated animals. TAE226 85-91 matrix metallopeptidase 10 Mus musculus 32-38 24915008-7 2014 Glomerular expression of MMP-9, MMP-10 and MMP-12 mRNAs was significantly reduced in TAE226 treated animals. TAE226 85-91 matrix metallopeptidase 12 Mus musculus 43-49 24860788-10 2014 We then treated mice xenografted with Ph+ leukemia cells with the FAK inhibitor TAE226 in combination with a BCR-ABL TKI nilotinib. TAE226 80-86 PTK2 protein tyrosine kinase 2 Mus musculus 66-69 24036212-9 2013 The FAK inhibitor TAE226 and the specific knockdown of Grb2 remarkably alleviated TGFbeta1-induced podocyte apoptosis. TAE226 18-24 PTK2 protein tyrosine kinase 2 Mus musculus 4-7 24036212-9 2013 The FAK inhibitor TAE226 and the specific knockdown of Grb2 remarkably alleviated TGFbeta1-induced podocyte apoptosis. TAE226 18-24 transforming growth factor, beta 1 Mus musculus 82-90 21454698-6 2011 Finally, our data indicate that FAK inhibitors could be used as potential therapeutic agents for patients with multiple endocrine neoplasia type 2 tumors because both, treatment with the FAK kinase inhibitor NVP-TAE226 and FAK down-regulation by siRNA reduced RET phosphorylation and signaling as well as the proliferation and survival of tumor and transfected cell lines expressing oncogenic RET. TAE226 212-218 protein tyrosine kinase 2 Homo sapiens 187-190 23845217-4 2013 X-ray crystallographic analysis of the co-crystal structure for compound 34 revealed that the mode of interaction with the FAK kinase domain is highly similar to that observed in the complex of TAE-226. TAE226 194-201 protein tyrosine kinase 2 Homo sapiens 123-126 22766511-0 2012 Anti-tumor effect of a novel FAK inhibitor TAE226 against human oral squamous cell carcinoma. TAE226 43-49 protein tyrosine kinase 2 Homo sapiens 29-32 22766511-2 2012 In order to seek therapies targeting oral squamous cell carcinoma, we developed the novel FAK Tyr(397) inhibitor TAE226 and investigated its anti-tumor effects and mechanisms. TAE226 113-119 protein tyrosine kinase 2 Homo sapiens 90-93 22766511-7 2012 In addition, TAE226 inhibited the expression of phospho-FAK Tyr(397) and phospho AKT Ser(473), resulting in caspase-mediated apoptosis. TAE226 13-19 protein tyrosine kinase 2 Homo sapiens 56-59 22766511-7 2012 In addition, TAE226 inhibited the expression of phospho-FAK Tyr(397) and phospho AKT Ser(473), resulting in caspase-mediated apoptosis. TAE226 13-19 AKT serine/threonine kinase 1 Homo sapiens 81-84 22766511-9 2012 CONCLUSIONS: Our results provide compelling evidence that FAK is critically involved in oral squamous cell carcinoma and that the FAK inhibitor TAE226 can potentially be effectively used for the treatment of oral squamous cell carcinoma. TAE226 144-150 protein tyrosine kinase 2 Homo sapiens 58-61 22766511-9 2012 CONCLUSIONS: Our results provide compelling evidence that FAK is critically involved in oral squamous cell carcinoma and that the FAK inhibitor TAE226 can potentially be effectively used for the treatment of oral squamous cell carcinoma. TAE226 144-150 protein tyrosine kinase 2 Homo sapiens 130-133 22705303-0 2012 Oral administration of FAK inhibitor TAE226 inhibits the progression of peritoneal dissemination of colorectal cancer. TAE226 37-43 PTK2 protein tyrosine kinase 2 Mus musculus 23-26 22705303-3 2012 Since we and other groups have reported that the inhibition of FAK activity exhibited a potent anticancer effect in several cancer models, we hypothesized that TAE226, a novel ATP-competitive tyrosine kinase inhibitor designed to target FAK, can prevent the occurrence and progression of peritoneal dissemination. TAE226 160-166 PTK2 protein tyrosine kinase 2 Mus musculus 63-66 22705303-3 2012 Since we and other groups have reported that the inhibition of FAK activity exhibited a potent anticancer effect in several cancer models, we hypothesized that TAE226, a novel ATP-competitive tyrosine kinase inhibitor designed to target FAK, can prevent the occurrence and progression of peritoneal dissemination. TAE226 160-166 PTK2 protein tyrosine kinase 2 Mus musculus 237-240 22705303-4 2012 In vitro, TAE226 greatly inhibited the proliferation and migration of HCT116 colon cancer cells, while their adhesion on the matrix surface was minimally inhibited when FAK activity and expression was suppressed by TAE226 and siRNA. TAE226 215-221 protein tyrosine kinase 2 Homo sapiens 169-172 22705303-8 2012 Taken together, a possible strategy for inhibiting peritoneal dissemination by targeting FAK with TAE226 appears to be applicable through anti-proliferative and anti-invasion/anti-migration mechanisms. TAE226 98-104 PTK2 protein tyrosine kinase 2 Mus musculus 89-92 23642017-3 2013 In the present study, we investigated whether the targeted inhibition of FAK by using a specific inhibitor, TAE226, has the potential to regulate pulmonary fibrosis. TAE226 108-114 PTK2 protein tyrosine kinase 2 Mus musculus 73-76 23642017-4 2013 TAE226 showed inhibitory activity of autophosphorylation of FAK at tyrosine 397 in lung fibroblasts. TAE226 0-6 PTK2 protein tyrosine kinase 2 Mus musculus 60-63 23642017-5 2013 The addition of TAE226 inhibited the proliferation of lung fibroblasts in response to various growth factors, including platelet-derived growth factor and insulin-like growth factor I, in vitro. TAE226 16-22 insulin-like growth factor 1 Mus musculus 155-183 21454698-6 2011 Finally, our data indicate that FAK inhibitors could be used as potential therapeutic agents for patients with multiple endocrine neoplasia type 2 tumors because both, treatment with the FAK kinase inhibitor NVP-TAE226 and FAK down-regulation by siRNA reduced RET phosphorylation and signaling as well as the proliferation and survival of tumor and transfected cell lines expressing oncogenic RET. TAE226 212-218 protein tyrosine kinase 2 Homo sapiens 32-35 21454698-6 2011 Finally, our data indicate that FAK inhibitors could be used as potential therapeutic agents for patients with multiple endocrine neoplasia type 2 tumors because both, treatment with the FAK kinase inhibitor NVP-TAE226 and FAK down-regulation by siRNA reduced RET phosphorylation and signaling as well as the proliferation and survival of tumor and transfected cell lines expressing oncogenic RET. TAE226 212-218 protein tyrosine kinase 2 Homo sapiens 187-190 21454698-6 2011 Finally, our data indicate that FAK inhibitors could be used as potential therapeutic agents for patients with multiple endocrine neoplasia type 2 tumors because both, treatment with the FAK kinase inhibitor NVP-TAE226 and FAK down-regulation by siRNA reduced RET phosphorylation and signaling as well as the proliferation and survival of tumor and transfected cell lines expressing oncogenic RET. TAE226 212-218 ret proto-oncogene Homo sapiens 260-263 21454698-6 2011 Finally, our data indicate that FAK inhibitors could be used as potential therapeutic agents for patients with multiple endocrine neoplasia type 2 tumors because both, treatment with the FAK kinase inhibitor NVP-TAE226 and FAK down-regulation by siRNA reduced RET phosphorylation and signaling as well as the proliferation and survival of tumor and transfected cell lines expressing oncogenic RET. TAE226 212-218 ret proto-oncogene Homo sapiens 393-396 19020730-0 2008 TAE226, a dual inhibitor for FAK and IGF-IR, has inhibitory effects on mTOR signaling in esophageal cancer cells. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 29-32 21338601-0 2011 Anti-tumor effect in human breast cancer by TAE226, a dual inhibitor for FAK and IGF-IR in vitro and in vivo. TAE226 44-50 protein tyrosine kinase 2 Homo sapiens 73-76 21338601-0 2011 Anti-tumor effect in human breast cancer by TAE226, a dual inhibitor for FAK and IGF-IR in vitro and in vivo. TAE226 44-50 insulin like growth factor 1 receptor Homo sapiens 81-87 21338601-3 2011 In this study, we have analyzed anti-tumor effects of the novel FAK Tyr(397) inhibitor TAE226 against bone metastasis in breast cancer by using TAE226. TAE226 87-93 protein tyrosine kinase 2 Homo sapiens 64-67 21338601-3 2011 In this study, we have analyzed anti-tumor effects of the novel FAK Tyr(397) inhibitor TAE226 against bone metastasis in breast cancer by using TAE226. TAE226 144-150 protein tyrosine kinase 2 Homo sapiens 64-67 21338601-7 2011 Moreover, TAE226 inhibited the receptor activator for nuclear factor kappa B Ligand (RANKL) gene expression induced by parathyroid hormone-related protein (PTHrP) in bone stromal ST2 cells and blood free calcium concentration induced by PTHrP administration in vivo. TAE226 10-16 TNF superfamily member 11 Homo sapiens 31-83 21338601-7 2011 Moreover, TAE226 inhibited the receptor activator for nuclear factor kappa B Ligand (RANKL) gene expression induced by parathyroid hormone-related protein (PTHrP) in bone stromal ST2 cells and blood free calcium concentration induced by PTHrP administration in vivo. TAE226 10-16 TNF superfamily member 11 Homo sapiens 85-90 21338601-7 2011 Moreover, TAE226 inhibited the receptor activator for nuclear factor kappa B Ligand (RANKL) gene expression induced by parathyroid hormone-related protein (PTHrP) in bone stromal ST2 cells and blood free calcium concentration induced by PTHrP administration in vivo. TAE226 10-16 parathyroid hormone like hormone Homo sapiens 119-154 21338601-7 2011 Moreover, TAE226 inhibited the receptor activator for nuclear factor kappa B Ligand (RANKL) gene expression induced by parathyroid hormone-related protein (PTHrP) in bone stromal ST2 cells and blood free calcium concentration induced by PTHrP administration in vivo. TAE226 10-16 parathyroid hormone like hormone Homo sapiens 156-161 21338601-7 2011 Moreover, TAE226 inhibited the receptor activator for nuclear factor kappa B Ligand (RANKL) gene expression induced by parathyroid hormone-related protein (PTHrP) in bone stromal ST2 cells and blood free calcium concentration induced by PTHrP administration in vivo. TAE226 10-16 parathyroid hormone like hormone Homo sapiens 237-242 19729215-0 2009 3D cell cultures of human head and neck squamous cell carcinoma cells are radiosensitized by the focal adhesion kinase inhibitor TAE226. TAE226 129-135 protein tyrosine kinase 2 Homo sapiens 97-118 19729215-2 2009 The aim of this study was to evaluate the radiosensitizing potential of the FAK inhibitor TAE226 in three-dimensional (3D) tumor cell cultures. TAE226 90-96 protein tyrosine kinase 2 Homo sapiens 76-79 19729215-6 2009 Intriguingly, TAE226 only significantly radiosensitized 3D HNSCC cell cultures accompanied by a pronounced dephosphorylation of FAK, Akt and ERK1/2. TAE226 14-20 protein tyrosine kinase 2 Homo sapiens 128-131 19729215-6 2009 Intriguingly, TAE226 only significantly radiosensitized 3D HNSCC cell cultures accompanied by a pronounced dephosphorylation of FAK, Akt and ERK1/2. TAE226 14-20 AKT serine/threonine kinase 1 Homo sapiens 133-136 19729215-6 2009 Intriguingly, TAE226 only significantly radiosensitized 3D HNSCC cell cultures accompanied by a pronounced dephosphorylation of FAK, Akt and ERK1/2. TAE226 14-20 mitogen-activated protein kinase 3 Homo sapiens 141-147 19729215-7 2009 CONCLUSIONS: Our data demonstrate TAE226 as potent FAK inhibitor that enhances the cellular radiosensitivity particularly of HNSCC cells grown in a 3D cell culture model. TAE226 34-40 protein tyrosine kinase 2 Homo sapiens 51-54 19139121-6 2009 When FAK activity in those cells was inhibited by TAE226, cell growth was equally suppressed and the cells underwent apoptosis regardless of the c-KIT mutation types. TAE226 50-56 PTK2 protein tyrosine kinase 2 Mus musculus 5-8 21338601-8 2011 These findings suggest that FAK was critically involved in osteolytic metastasis and activated in tumors, pre-osteoclasts, mature osteoclasts, and bone stromal cells and TAE226 can be effectively used for the treatment of cancer induced bone metastasis and other bone diseases. TAE226 170-176 protein tyrosine kinase 2 Homo sapiens 28-31 21347357-11 2011 A FAK selective inhibitor TAE-226, blocked TXA(2) generation. TAE226 26-33 PTK2 protein tyrosine kinase 2 Mus musculus 2-5 19784551-0 2010 TAE226-mediated inhibition of focal adhesion kinase interferes with tumor angiogenesis and vasculogenesis. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 30-51 19784551-4 2010 In the current study we analyzed the anti-angiogenic properties of the FAK inhibitor TAE226 on the proliferation of blood outgrowth endothelial cell (OEC) and differentiation of endothelial progenitor cells (EPC), derived from peripheral blood CD133(+) cells, tube formation and on neovascularization in a HT29 xenotransplant model. TAE226 85-91 protein tyrosine kinase 2 Homo sapiens 71-74 19784551-12 2010 Since TAE226 has been shown to inhibit the PI3 kinase, Akt kinase, mTor pathway, addition of RAD001 may not increase this effect. TAE226 6-12 mechanistic target of rapamycin kinase Homo sapiens 67-71 20441998-5 2010 Infections were reduced in the presence of the FAK inhibitor, TAE226. TAE226 62-68 protein tyrosine kinase 2 Homo sapiens 47-50 19020730-9 2008 TAE226 inhibited the expression of mTOR, Akt, p70S6K and S6 as well as the phosphorylation of mTOR (Ser2448), Akt (Ser473), p70S6K (Thr389) and S6 (Ser240/244). TAE226 0-6 mechanistic target of rapamycin kinase Homo sapiens 35-39 19020730-9 2008 TAE226 inhibited the expression of mTOR, Akt, p70S6K and S6 as well as the phosphorylation of mTOR (Ser2448), Akt (Ser473), p70S6K (Thr389) and S6 (Ser240/244). TAE226 0-6 AKT serine/threonine kinase 1 Homo sapiens 41-44 19020730-9 2008 TAE226 inhibited the expression of mTOR, Akt, p70S6K and S6 as well as the phosphorylation of mTOR (Ser2448), Akt (Ser473), p70S6K (Thr389) and S6 (Ser240/244). TAE226 0-6 ribosomal protein S6 kinase B1 Homo sapiens 46-52 19020730-9 2008 TAE226 inhibited the expression of mTOR, Akt, p70S6K and S6 as well as the phosphorylation of mTOR (Ser2448), Akt (Ser473), p70S6K (Thr389) and S6 (Ser240/244). TAE226 0-6 mechanistic target of rapamycin kinase Homo sapiens 94-98 19020730-9 2008 TAE226 inhibited the expression of mTOR, Akt, p70S6K and S6 as well as the phosphorylation of mTOR (Ser2448), Akt (Ser473), p70S6K (Thr389) and S6 (Ser240/244). TAE226 0-6 AKT serine/threonine kinase 1 Homo sapiens 110-113 19020730-9 2008 TAE226 inhibited the expression of mTOR, Akt, p70S6K and S6 as well as the phosphorylation of mTOR (Ser2448), Akt (Ser473), p70S6K (Thr389) and S6 (Ser240/244). TAE226 0-6 ribosomal protein S6 kinase B1 Homo sapiens 124-130 19020730-11 2008 Together, these data show that TAE226 has potent inhibitory effects on mTOR signaling and esophageal cancer cell growth indicating that TAE226 has potential application in esophageal cancer treatment. TAE226 31-37 mechanistic target of rapamycin kinase Homo sapiens 71-75 19020730-11 2008 Together, these data show that TAE226 has potent inhibitory effects on mTOR signaling and esophageal cancer cell growth indicating that TAE226 has potential application in esophageal cancer treatment. TAE226 136-142 mechanistic target of rapamycin kinase Homo sapiens 71-75 19020730-0 2008 TAE226, a dual inhibitor for FAK and IGF-IR, has inhibitory effects on mTOR signaling in esophageal cancer cells. TAE226 0-6 insulin like growth factor 1 receptor Homo sapiens 37-43 19020730-0 2008 TAE226, a dual inhibitor for FAK and IGF-IR, has inhibitory effects on mTOR signaling in esophageal cancer cells. TAE226 0-6 mechanistic target of rapamycin kinase Homo sapiens 71-75 19020730-4 2008 TAE226, a novel small molecule compound, is a potent ATP competitive inhibitor of FAK and IGF-IR. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 82-85 19020730-4 2008 TAE226, a novel small molecule compound, is a potent ATP competitive inhibitor of FAK and IGF-IR. TAE226 0-6 insulin like growth factor 1 receptor Homo sapiens 90-96 19020730-5 2008 TAE226 can block FAK and IGF-IR signaling pathways. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 17-20 19020730-5 2008 TAE226 can block FAK and IGF-IR signaling pathways. TAE226 0-6 insulin like growth factor 1 receptor Homo sapiens 25-31 19020730-6 2008 The purpose of this study was to explore the inhibitory effects on mTOR signaling and the mechanism of cell growth suppression by TAE226. TAE226 130-136 mechanistic target of rapamycin kinase Homo sapiens 67-71 19030106-0 2008 Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. TAE226 53-59 protein tyrosine kinase 2 Homo sapiens 26-29 18259944-2 2008 TAE226 is a novel small molecule FAK inhibitor. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 33-36 18259944-6 2008 RESULTS: Treatment of human neuroblastoma cell lines with TAE226 resulted in a concentration dependent decrease in FAK phosphorylation, decrease in cellular viability, cell cycle arrest, and an increase in apoptosis. TAE226 58-64 protein tyrosine kinase 2 Homo sapiens 115-118 17849451-0 2008 TAE226-induced apoptosis in breast cancer cells with overexpressed Src or EGFR. TAE226 0-6 epidermal growth factor receptor Homo sapiens 74-78 17849451-4 2008 In the present study, we studied the effect of a novel FAK inhibitor, TAE226 (Novartis, Inc.), on the breast cancer cell lines. TAE226 70-76 protein tyrosine kinase 2 Homo sapiens 55-58 17849451-7 2008 The TAE226 drug caused a dose-dependent increase of detachment and apoptosis in both BT474 and MCF-7-Vector and Src cells and in BT474-EGFR and BT474-pcDNA3 cells. TAE226 4-10 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 112-115 17849451-7 2008 The TAE226 drug caused a dose-dependent increase of detachment and apoptosis in both BT474 and MCF-7-Vector and Src cells and in BT474-EGFR and BT474-pcDNA3 cells. TAE226 4-10 epidermal growth factor receptor Homo sapiens 129-139 17849451-8 2008 Additionally, TAE226 caused downregulation of Y397-FAK, FAK and activation of PARP or caspase-3 proteins. TAE226 14-20 protein tyrosine kinase 2 Homo sapiens 51-54 17849451-8 2008 Additionally, TAE226 caused downregulation of Y397-FAK, FAK and activation of PARP or caspase-3 proteins. TAE226 14-20 protein tyrosine kinase 2 Homo sapiens 56-59 17849451-8 2008 Additionally, TAE226 caused downregulation of Y397-FAK, FAK and activation of PARP or caspase-3 proteins. TAE226 14-20 poly(ADP-ribose) polymerase 1 Homo sapiens 78-82 17849451-8 2008 Additionally, TAE226 caused downregulation of Y397-FAK, FAK and activation of PARP or caspase-3 proteins. TAE226 14-20 caspase 3 Homo sapiens 86-95 17849451-11 2008 Thus, inhibition of autophosphorylation activity of FAK with the TAE226 inhibitor at 10-20 microM is effective in causing apoptosis in breast cancer cells, resistant to the Ad-FAK-CD inhibitor that can be used effectively in therapy. TAE226 65-71 protein tyrosine kinase 2 Homo sapiens 52-55 17849451-11 2008 Thus, inhibition of autophosphorylation activity of FAK with the TAE226 inhibitor at 10-20 microM is effective in causing apoptosis in breast cancer cells, resistant to the Ad-FAK-CD inhibitor that can be used effectively in therapy. TAE226 65-71 protein tyrosine kinase 2 Homo sapiens 176-179 18628478-4 2008 Cultured esophageal adenocarcinoma cells were treated with TAE226, a specific FAK inhibitor with an additional effect of inhibiting insulin-like growth factor-I receptor (IGF-IR), to assess its anticancer effect in vitro. TAE226 59-65 protein tyrosine kinase 2 Homo sapiens 78-81 18628478-9 2008 The activities of FAK, IGF-IR, and AKT were suppressed by TAE226 and subsequent dephosphorylation of BAD at Ser(136) occurred, resulting in caspase-mediated apoptosis. TAE226 58-64 protein tyrosine kinase 2 Homo sapiens 18-21 18628478-9 2008 The activities of FAK, IGF-IR, and AKT were suppressed by TAE226 and subsequent dephosphorylation of BAD at Ser(136) occurred, resulting in caspase-mediated apoptosis. TAE226 58-64 insulin like growth factor 1 receptor Homo sapiens 23-29 18628478-9 2008 The activities of FAK, IGF-IR, and AKT were suppressed by TAE226 and subsequent dephosphorylation of BAD at Ser(136) occurred, resulting in caspase-mediated apoptosis. TAE226 58-64 AKT serine/threonine kinase 1 Homo sapiens 35-38 18628478-11 2008 CONCLUSIONS: These results suggest that TAE226, a dual tyrosine kinase inhibitor for FAK and IGF-IR, could become a new remedy for Barrett"s esophageal adenocarcinoma. TAE226 40-46 protein tyrosine kinase 2 Homo sapiens 85-88 18628478-11 2008 CONCLUSIONS: These results suggest that TAE226, a dual tyrosine kinase inhibitor for FAK and IGF-IR, could become a new remedy for Barrett"s esophageal adenocarcinoma. TAE226 40-46 insulin like growth factor 1 receptor Homo sapiens 93-99 17849451-0 2008 TAE226-induced apoptosis in breast cancer cells with overexpressed Src or EGFR. TAE226 0-6 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 67-70 19030106-3 2008 Recently, a novel bis-anilino pyrimidine inhibitor, TAE226, was reported to efficiently inhibit FAK signaling, arrest tumor growth and invasion and prolong the life of mice with glioma or ovarian tumor implants. TAE226 52-58 PTK2 protein tyrosine kinase 2 Mus musculus 96-99 19030106-4 2008 Here we describe the crystal structures of the FAK kinase bound to TAE226 and three related bis-anilino pyrimidine compounds. TAE226 67-73 protein tyrosine kinase 2 Homo sapiens 47-50 19030106-5 2008 TAE226 induces a conformation of the N-terminal portion of the kinase activation loop that is only observed in FAK, but is distinct from the conformation in both the active and inactive states of the kinase. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 111-114 19030106-7 2008 The presence of a glycine residue in this position contributes to the specificity of TAE226 and related compounds for FAK. TAE226 85-91 protein tyrosine kinase 2 Homo sapiens 118-121 18006843-0 2007 Therapeutic efficacy of a novel focal adhesion kinase inhibitor TAE226 in ovarian carcinoma. TAE226 64-70 protein tyrosine kinase 2 Homo sapiens 32-53 18006843-2 2007 In the current study, we characterized the biological and therapeutic effects of a novel FAK inhibitor, TAE226. TAE226 104-110 protein tyrosine kinase 2 Homo sapiens 89-92 18006843-5 2007 In vitro, TAE226 inhibited the phosphorylation of FAK at both Y397 and Y861 sites, inhibited cell growth in a time- and dose-dependent manner, and enhanced docetaxel-mediated growth inhibition by 10- and 20-fold in the taxane-sensitive and taxane-resistant cell lines, respectively. TAE226 10-16 protein tyrosine kinase 2 Homo sapiens 50-53 18006843-6 2007 In vivo, FAK inhibition by TAE226 significantly reduced tumor burden in the HeyA8, SKOV3ip1, and HeyA8-MDR models (46-64%) compared with vehicle-treated controls. TAE226 27-33 protein tyrosine kinase 2 Homo sapiens 9-12 18006843-11 2007 The novel FAK inhibitor, TAE226, offers an attractive therapeutic approach in ovarian carcinoma. TAE226 25-31 protein tyrosine kinase 2 Homo sapiens 10-13 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 77-83 protein tyrosine kinase 2 Homo sapiens 55-58 17219439-0 2007 A novel low-molecular weight inhibitor of focal adhesion kinase, TAE226, inhibits glioma growth. TAE226 65-71 protein tyrosine kinase 2 Homo sapiens 42-63 17219439-7 2007 As all glioma cell lines examined expressed phosphorylated FAK, we examined the efficacy of a novel low-molecular weight inhibitor of FAK, TAE226, against human glioma cell lines. TAE226 139-145 protein tyrosine kinase 2 Homo sapiens 134-137 17219439-8 2007 TAE226 inhibited the phosphorylation of FAK as well as the downstream effectors AKT, extracellular signal-related kinase, and S6 ribosomal protein in multiple glioma cell lines. TAE226 0-6 protein tyrosine kinase 2 Homo sapiens 40-43 17219439-8 2007 TAE226 inhibited the phosphorylation of FAK as well as the downstream effectors AKT, extracellular signal-related kinase, and S6 ribosomal protein in multiple glioma cell lines. TAE226 0-6 AKT serine/threonine kinase 1 Homo sapiens 80-83 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 77-83 insulin like growth factor 1 receptor Homo sapiens 63-69 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 77-83 protein tyrosine kinase 2 Homo sapiens 153-156 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 77-83 insulin like growth factor 1 receptor Homo sapiens 161-167 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 102-108 protein tyrosine kinase 2 Homo sapiens 55-58 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 102-108 insulin like growth factor 1 receptor Homo sapiens 63-69 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 102-108 protein tyrosine kinase 2 Homo sapiens 153-156 17431114-4 2007 We hypothesized that inhibiting the phosphorylation of FAK and IGF-IR by NVP-TAE226 (hereafter called TAE226), a novel dual tyrosine kinase inhibitor of FAK and IGF-IR, would suppress the growth and invasion of glioma cells. TAE226 102-108 insulin like growth factor 1 receptor Homo sapiens 161-167 17431114-5 2007 In culture, TAE226 inhibited extracellular matrix-induced autophosphorylation of FAK (Tyr(397)). TAE226 12-18 protein tyrosine kinase 2 Homo sapiens 81-84 17431114-6 2007 TAE226 also inhibited IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. TAE226 0-6 insulin like growth factor 1 Homo sapiens 22-27 17431114-6 2007 TAE226 also inhibited IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. TAE226 0-6 insulin like growth factor 1 receptor Homo sapiens 55-61 17431114-6 2007 TAE226 also inhibited IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. TAE226 0-6 AKT serine/threonine kinase 1 Homo sapiens 123-126 17431114-7 2007 TAE226 retarded tumor cell growth as assessed by a cell viability assay and attenuated G(2)-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr(15)) protein expression. TAE226 0-6 cyclin B1 Homo sapiens 147-156 17431114-7 2007 TAE226 retarded tumor cell growth as assessed by a cell viability assay and attenuated G(2)-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr(15)) protein expression. TAE226 0-6 cyclin dependent kinase 1 Homo sapiens 176-180 17431114-9 2007 Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibited G(2)-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis. TAE226 15-21 tumor protein p53 Homo sapiens 68-71 17431114-10 2007 Induction of apoptosis by TAE226 was substantiated by detection of caspase-3/7 activation and poly(ADP-ribose) polymerase cleavage and by an Annexin V apoptosis assay. TAE226 26-32 caspase 3 Homo sapiens 67-76 17431114-10 2007 Induction of apoptosis by TAE226 was substantiated by detection of caspase-3/7 activation and poly(ADP-ribose) polymerase cleavage and by an Annexin V apoptosis assay. TAE226 26-32 annexin A5 Homo sapiens 141-150 17431114-12 2007 Collectively, these data show that blocking the signaling pathways of FAK and IGF-IR with TAE226 has the potential to be an efficacious treatment for human gliomas. TAE226 90-96 protein tyrosine kinase 2 Homo sapiens 70-73 17431114-12 2007 Collectively, these data show that blocking the signaling pathways of FAK and IGF-IR with TAE226 has the potential to be an efficacious treatment for human gliomas. TAE226 90-96 insulin like growth factor 1 receptor Homo sapiens 78-84