MK2461

Description	MK-2461 is a potent inhibitor of Met, Ron, Flt1, Flt 3, PDGFRβ, and Mer with IC50 of 2.5 nM, 7 nM, 10 nM, 22 nM, 22 nM and 24 nM, respectively.MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met. MK-2461 inhibited in vitro phosphorylation of a peptide substrate recognized by wild-type or oncogenic c-Met kinases (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC50 values of 0.4 to 2.5 nmol/L. In tumor cells, MK-2461 effectively suppressed constitutive or ligand-induced phosphorylation of the juxtamembrane domain and COOH-terminal docking site of c-Met, and its downstream signaling to the phosphoinositide 3-kinaseÂ–AKT and RasÂ–extracellular signal-regulated kinase pathways, without inhibiting autophosphorylation of the c-Met activation loop. In cell culture, MK-2461 inhibited hepatocyte growth factor/c-MetÂ–dependent mitogenesis, migration, cell scatter, and tubulogenesis. In a murine xenograft model of c-MetÂ–dependent gastric cancer, a well-tolerated oral regimen of MK-2461 administered at 100 mg/kg twice daily effectively suppressed c-Met signaling and tumor growth.
Pathways	Angiogenesis/Protein Tyrosine Kinase
Targets	c Met

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