MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}
产品描述
A selective class I c-Met kinase inhibitor (Ki = 4.8 nM) that inhibits tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM); shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop
