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MK-2461 Sale

目录号 : GC16337

A c-MET inhibitor

MK-2461 Chemical Structure

Cas No.:917879-39-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,418.00
现货
5mg
¥1,397.00
现货
10mg
¥2,279.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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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.

Chemical Properties

Cas No. 917879-39-1 SDF
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 SMILES CN1C=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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.018 mL 10.0898 mL 20.1796 mL
5 mM 0.4036 mL 2.018 mL 4.0359 mL
10 mM 0.2018 mL 1.009 mL 2.018 mL
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