PF-04217903

PF-04217903 is a novel ATP-competitive small-molecule inhibitor of c-Met kinase. PF-04217903 displays more than 1,000-fold selectivity for c-Met compared with more than 150 kinases. PF-04217903 inhibits tumor cell proliferation, survival, migration/invasion in MET-amplified cell lines in vitro and shows marked antitumor activity in tumor models harboring either MET gene amplification or a hepatocyte growth factor (HGF)/c-Met autocrine loop at well-tolerated dose levels in vivo.