PHA-665752

PHA-665752 is a potent, selective, and ATP-competitive small molecule inhibitor of the c-Met receptor tyrosine kinase (also known as MET or hepatocyte growth factor receptor). It exhibits an IC50 of 9 nM for c-Met in cell-free assays and demonstrates over 50-fold selectivity for c-Met compared to other related kinases[1][2][4][5]. The compound inhibits phosphorylation of c-Met and its downstream signaling pathways, leading to reduced cell proliferation, motility, invasion, and induction of apoptosis in various cancer cell lines including lung, gastric, pancreatic carcinoma cells[3][5]. In vivo studies show that PHA-665752 suppresses tumor growth in xenograft models by inhibiting tumorigenicity and angiogenesis[2][3][6]. It has been used primarily as a research tool to study MET-driven cancers. The drug was developed by Pfizer.

Other names

PHA 665752PHA665752PHA-665752