产品描述:
MK-2461 is an inhibitor of wild-type and mutant forms of c-MET (IC50s = 0.4-2 nM).{61218} It is selective for c-MET over a panel of 13 additional kinases (IC50s = 22-7,800 nM) but does inhibit Ron and FLT1 (IC50s = 7 and 10 nM, respectively). MK-2461 also inhibits autophosphorylation of FGFR2 and PDGFRα in KATO III cells but not EGF-induced phosphorylation of EGFR in A549 lung cancer cells when used at a concentration of 2 µM.{61219} It reduces proliferation in a panel of cancer cell lines, including cells expressing constitutively active c-MET, FGFR2, or PDGFR (IC50s = ≤1 µM for all).{61219} MKT-2461 (10-200 mg/kg) reduces tumor growth in a GTL-16 gastric cancer mouse xenograft model.{61218}