PHA-665752

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PHA-665752 is a small-molecule inhibitor of c-Met, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. c-Met is a tyrosine kinase receptor for hepatocyte growth factor/scatter factor (HGF/SF). PHA665752 inhibited specific phosphorylation of TPR-MET as well as phosphorylation of downstream targets of the mammalian target of rapamycin pathway. Short-term treatment with PHA-665752 decreased the numbers of premalignant lung lesions and induced apoptosis in tumor cells and vascular endothelial cells within lesions. In cell culture, PHA-665752 induced apoptosis of a lung adenocarcinoma cell line derived from Kras(LA1) mice (LKR-13) and a murine lung endothelial cell line (MEC). PHA665752 was shown to inhibit cMet/HGF/SF signaling in vitro, suggesting c-Met inhibitors may have efficacy for blocking local progression and/or metastatic spread of c-Met-positive NBL in vivo.

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