MK-2461

MK-2461 is a potent, orally bioavailable small molecule inhibitor that targets multiple receptor tyrosine kinases, with primary activity against c-Met (hepatocyte growth factor receptor), including both wild-type and mutant forms. It acts as an ATP-competitive inhibitor and demonstrates high selectivity for activated c-Met (IC50 = 0.4–2.5 nM), but also inhibits other kinases such as FGFRs (fibroblast growth factor receptors), PDGFRβ (platelet-derived growth factor receptor beta), KDR (VEGFR2), TrkA/B, Flt3/4/1, Ron, and Mer at higher concentrations[1][2][3][7]. In preclinical studies and early clinical trials for advanced solid tumors and multiple myeloma, MK-2461 suppressed tumor cell proliferation by blocking downstream signaling pathways including PI3K-AKT and Ras-MAPK[2][6]. The drug was developed primarily for cancer therapy in tumors with MET or FGFR2 amplification or activation[2][3]. Its maximum clinical trial phase reached Phase II across all indications[4].

Other names

917879-39-1UNII-4200RD53XFUNII4200RD53XFUNII 4200RD53XF