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Supplementary Figures from In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models

Authors :
Angela Coxon
Isabelle Dussault
Richard Kendall
Robert Radinsky
Jean-Christophe Harmange
Deborah M. Choquette
Daniel Baker
Michael A. Damore
Jonathan Werner
Jodi Moriguchi
Paula J. Kaplan-Lefko
Benny Amore
Teresa L. Burgess
Hue T. Kha
Martin A. Broome
Yihong Zhang
Yajing Yang
Sean Caenepeel
Karen Rex
Paul E. Hughes
Publication Year :
2023
Publisher :
American Association for Cancer Research (AACR), 2023.

Abstract

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 the phosphorylation of MET and but not its downstream effectors in MET-amplified, KRAS mutant NSCLC cell line NCI-H1573; Figure S4. Cell lines harboring MET FISH scores >3 exhibited sensitivity to AMG 337. MET FISH analysis was performed on a subset of cancer cell lines exhibiting elevated MET gene copy number; Figure S5. Selective inhibition of MET exhibits partial effects on the viability of U-87 MG glioblastoma cells harboring an HGF/MET autocrine loop; Figure S6. Increases in MET gene number correlate with high levels of total MET protein; Figure S7. AMG 337 inhibits Gab-1 phosphorylation in a concentration dependent manner in the TPR-MET mouse tumor model.

Details

Database :
OpenAIRE
Accession number :
edsair.doi.dedup.....a17dda613dc16280ece0a724bc5ba127
Full Text :
https://doi.org/10.1158/1535-7163.22507710