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. EMD 1214063 inhibits c-Met with an IC50 value of 3 nM, demonstrating at least 1,000-fold selectivity for c-Met over a panel of 242 additional kinases. It has been shown to inhibit c-Met phosphorylation and downstream signaling in various cancer cell lines (IC50s = 6-9 nM) and, at 5-15 mg/kg, to regress tumors in mouse xenograft models.
