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MK-2461
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK-2461图片
CAS NO:917879-39-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
MK-2461 是一种新型的 ATP 竞争性多靶点活化 c-Met 抑制剂,平均 IC50 为 2.5 nM。
Cas No.917879-39-1
化学名9-[[[(2R)-1,4-dioxan-2-yl]methyl-methylsulfamoyl]amino]-2-(1-methylpyrazol-4-yl)-11-oxobenzo[1,2]cyclohepta[2,4-b]pyridine
Canonical SMILESCN1C=C(C=N1)C2=CN=C3C=CC4=C(C=C(C=C4)NS(=O)(=O)N(C)CC5COCCO5)C(=O)C3=C2
分子式C24H25N5O5S
分子量495.55
溶解度≥ 24.8mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MK-2461 is a potent inhibitor of Met, Flt1, Flt 3, Ron, PDGFRβ, and Mer with IC50 of 2.5 nM, 10 nM, 22 nM, 7 nM, and 24 nM, respectively.

c-Met, also named as hepatocyte growth factor receptor (HGFR) is a receptor tyrosine kinase that is essential for embryonic development and would healing. In many tumor cells, this molecular is overexpressed or mutated and was found to play important roles in tumor cell proliferation, survival, invasion, metastasis and angiogenesis.

In vitro, MK-2461treatment blocked hepatocyte growth factor/c-Met- dependent mitogenesis, migration, cell scatter, and tubulogenesis 1.

In a murine xenograft model of c-Met-dependent gastric cancer, oral administration of MK-2461 at a dosge of 100 mg/kg twice daily effectively inhibited c-Met signaling and tumor growth 1. Consistently, MK-2461 inhibited the tumor growth which was formed by s.c. injection of mouse NIH-3T3 cells expressing oncogenic c-Met mutants 1. These evidence support the preclinical development of MK-2461 for cancer therapy.

Reference:
1.   Pan BS, Chan GK, Chenard M, et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer research. 2010;70(4):1524-1533.