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Chemical Structure : MK-2461
CAS No.: 917879-39-1
Catalog No.: PC-45848Not For Human Use, Lab Use Only.
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $148 | In stock | |
| 10 mg | $228 | In stock | |
| 25 mg | $378 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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).
MK-2461 is 8- to 30-fold less sensitive to FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB.
MK-2461 is equally or more potent against 5 c-Met mutants (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC50 of 0.4-2.5 nM.
MK-2461 inhibits c-Met-dependent mitogenesis, migration, cell scatter, and tubulogenesis in cells.
MK-2461 suppresses tumor growth a murine xenograft model of c-Met-dependent gastric cancer; orally active.
| M.Wt | 495.5508 | |
| Formula | C24H25N5O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 31 mg/mL |
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| Chemical Name/SMILES |
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]- |
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1. Pan BS, et al. Cancer Res. 2010 Feb 15;70(4):1524-33.
2. Rickert KW, et al. J Biol Chem. 2011 Apr 1;286(13):11218-25.
3. Katz JD, et al. J Med Chem. 2011 Jun 23;54(12):4092-108.
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