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View article: LKB1 regulates JNK-dependent stress signaling and apoptotic dependency of KRAS-mutant lung cancers
LKB1 regulates JNK-dependent stress signaling and apoptotic dependency of KRAS-mutant lung cancers Open
The efficacy of molecularly targeted therapies may be limited by co-occurring mutations within a tumor. Conversely, these alterations may confer collateral vulnerabilities that can be therapeutically leveraged. KRAS -mutant lung cancers ar…
View article: Identification of Structurally Novel KRAS<sup>G12C</sup> Inhibitors through Covalent DNA-Encoded Library Screening
Identification of Structurally Novel KRAS<sup>G12C</sup> Inhibitors through Covalent DNA-Encoded Library Screening Open
Covalent inhibition of the KRASG12C oncoprotein has emerged as a promising therapeutic approach for the treatment of nonsmall cell lung cancer (NSCLC). The identification of KRASG12C inhibitors has typically relied on the high-throughput s…
View article: Supplementary Figure S7 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S7 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S7 shows pathway alterations downstream of Tie2 and c-MET inhibition.
View article: Supplementary Figure S6 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S6 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S6 shows additional data on E-Cadherin protein expression.
View article: Supplementary Figures from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Figures from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
Figure S1. Kinase interaction map for AMG 337; Figure S2. In a large unbiased cancer cell line viability screen only MET-amplified cell lines were sensitive to treatment with an analogue of AMG 337 (Compound 5); Figure S3: AMG 337 inhibits…
View article: Data from Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma
Data from Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma Open
Aberrant hepatocyte growth factor (HGF)/MET signaling has been implicated in hepatocarcinogenesis, suggesting that MET may serve as an attractive therapeutic target in hepatocellular carcinoma. We sought to investigate the in vitro and in …
View article: Supplementary Figure S4 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S4 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S4 shows the effect of combination on lung metastases.
View article: Supplementary methods from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary methods from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
Supplementary methods of tumor xenograft studies and light microscopic evaluation of tumor xenografts
View article: Supplementary Figure S9 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S9 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S9 shows TIE2 and macrophage markers expression.
View article: Supplementary Figure S1 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S1 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S1 shows the chemical structure of compound 22.
View article: Supplementary Figure S6 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S6 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S6 shows additional data on E-Cadherin protein expression.
View article: Supplementary Figure S8 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S8 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S8 shows pTie expression in treated tumors.
View article: Supplementary Table S1 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Table S1 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
Enzymatic and cellular potency of Amgen Compound 5
View article: Supplementary Figure 1 from Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma
Supplementary Figure 1 from Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma Open
Western blot analysis in responsive PDX model (LI0612) after 14 days treatment. Total and phosphorylated levels of the indicated proteins were evaluated to assess the effects of AMG 337 on MET signaling. Five to twelve PDX samples were pro…
View article: Supplementary Data File 1 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Data File 1 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
AMG 337 KINOME scan binding data
View article: Supplementary Data File 2 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Data File 2 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
Tumor cell line profiling data
View article: Supplementary Figure S5 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S5 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S5 shows the effect of combination on E-Cadherin and Snail expression.
View article: Supplementary Figure S2 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S2 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S2 shows additional tumor growth data
View article: Supplementary Table S2 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Table S2 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
High-level focal amplification of MET is associated with sensitivity to AMG 337
View article: Supplementary Figure S9 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S9 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S9 shows TIE2 and macrophage markers expression.
View article: Supplementary Figure S3 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S3 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S3 shows additional tumor growth data
View article: Data from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Data from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
The MET receptor tyrosine kinase is involved in cell growth, survival, and invasion. Clinical studies with small molecule MET inhibitors have shown the role of biomarkers in identifying patients most likely to benefit from MET-targeted the…
View article: Supplementary Table S2 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Table S2 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
High-level focal amplification of MET is associated with sensitivity to AMG 337
View article: Data from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Data from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Receptor tyrosine kinase inhibitors have shown clinical benefit in clear cell renal cell carcinoma (ccRCC), but novel therapeutic strategies are needed. The angiopoietin/Tie2 and MET pathways have been implicated in tumor angiogenesis, met…
View article: Supplementary Figure S3 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S3 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S3 shows additional tumor growth data
View article: Supplementary Figure S8 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S8 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S8 shows pTie expression in treated tumors.
View article: Supplementary Table S1 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models
Supplementary Table S1 from <i>In Vitro</i> and <i>In Vivo</i> Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models Open
Enzymatic and cellular potency of Amgen Compound 5
View article: Supplementary Figure S5 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S5 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S5 shows the effect of combination on E-Cadherin and Snail expression.
View article: Supplementary Figure S10 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma
Supplementary Figure S10 from Dual Inhibition of Angiopoietin-TIE2 and MET Alters the Tumor Microenvironment and Prolongs Survival in a Metastatic Model of Renal Cell Carcinoma Open
Supplementary Figure S10 additional data on TIE2 and macrophage marker expression.