MK-2461

Research use only, not for human use.

MK-2461 is a potent multitargeted kinase inhibitor that preferentially inhibits c-Met with IC50 of 2.5 nM.

MK-2461 is a potent multitargeted kinase inhibitor that preferentially inhibits c-Met with IC50 of 2.5 nM, with similar potencies for Ron and Flt1 (IC50=7 and 10 nM, respectively); 8- to 30-fold less sensitive to FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB; is equally or more potent against 5 c-Met mutants (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC50 of 0.4-2.5 nM; inhibits c-Met-dependent mitogenesis, migration, cell scatter, and tubulogenesis in cells; suppresses tumor growth a murine xenograft model of c-Met-dependent gastric cancer; orally active.Solid Tumors Phase 2 Clinical

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MK 2461 | MK2461

Angiogenesis

c-Met/HGFR

c-Met(M1250T)|c-Met(N1100)|c-Met(Y1230C)|c-Met(Y1230H)|c-Met(Y1235D)

Cancer

Solid Tumors

917879-39-1

495.5508

C24H25N5O5S

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=S(NC1=CC=C2C(C(C3=CC(C4=CN(C)N=C4)=CN=C3C=C2)=O)=C1)(N(C[C@H]5OCCOC5)C)=O

Sulfamide, N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N'-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-

(-20℃)

With Ice Pack

≥ 2 years