MK-2461 |CAS:917879-39-1 Probechem Biochemicals

Chemical Structure : MK-2461

CAS No.: 917879-39-1

MK-2461 (MK 2461;MK2461)

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).

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5 mg	$148	In stock
10 mg	$228	In stock
25 mg	$378	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	495.5508
Formula	C24H25N5O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 31 mg/mL
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]-

References

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.

MK-2461 (MK 2461;MK2461)

Biological Activity

Physicochemical Properties

References

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