[CAS NO. 917879-39-1]  MK-2461

MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM. IC50 value: 2.5 nM [1] Target: c-Met in vitro: MK-2461 inhibits the kinase activity of human c-Met with a mean IC50 of 2.5 nM in the presence of 50 μM ATP. Ron (IC50 = 7 nM) and Flt1 (IC50 = 10 nM) are inhibited by MK-2461 with similar potencies to c-Met (IC50 = 2.5 nM), whereas nine other kinases, including FGFR1 , FGFR2 , FGFR3 , PDGFRβ , KDR, Flt3 , Flt4, TrkA , and TrkB , are found to be 8- to 30-fold less sensitive to MK-2461 than c-Met. [1] in vivo: MK-2461 inhibits c-Met signaling and tumor growth in tumor xenograft models in mice.[1]