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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Met (HGFR)-MK-2461
MK-2461

Chemical Structure : MK-2461

CAS No.: 917879-39-1

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MK-2461 (MK 2461;MK2461)

货号: 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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10 mg ￥2280 In stock
25 mg ￥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 495.5508
分子式 C24H25N5O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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]-

参考文献

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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