448101
Met Kinase Inhibitor
The Met Kinase Inhibitor, also referenced under CAS 658084-23-2, controls the biological activity of Met Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Met Kinase Inhibitor, (3Z)-N-(3-Chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide, SU11274
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About This Item
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质量水平
方案
≥98% (HPLC)
表单
powder
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
orange
溶解性
DMSO: 1 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C28H30ClN5O4S/c1-17-25(30-18(2)26(17)28(36)34-12-10-32(3)11-13-34)16-23-22-15-21(8-9-24(22)31-27(23)35)39(37,38)33(4)20-7-5-6-19(29)14-20/h5-9,14-16,30H,10-13H2,1-4H3,(H,31,35)/b23-16-
InChI key
FPYJSJDOHRDAMT-KQWNVCNZSA-N
一般描述
A cell-permeable pyrrole indolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Met kinase activity (IC50 = 20 nM). Exhibits >60-fold selectivity over Flk and >400-fold selectivity over Ron, FGFR-1, c-Src, Cdk2, PDGFRβ, EGFR, and Tie-2. Shown to inhibit HGF/SF-stimulated cellular signaling and Met-mediated tumorigenesis in various cancer cell lines.
生化/生理作用
Cell permeable: yes
Primary Target
met kinase activity
met kinase activity
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM against Met kinase activity
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
制备说明
Warm as needed for complete solubilization.
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Ma. P. C., et al. 2005. Cancer Res.65, 1479.
Berthou, S., et al. 2004. Oncogene23, 5387.
Wang, X., et al. 2003. Mol. Cancer Ther.2, 1085.
Sattler, M., et al. 2003. Cancer Res.63, 5462.
Berthou, S., et al. 2004. Oncogene23, 5387.
Wang, X., et al. 2003. Mol. Cancer Ther.2, 1085.
Sattler, M., et al. 2003. Cancer Res.63, 5462.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Sylvie Berthou et al.
Oncogene, 23(31), 5387-5393 (2004-04-06)
Point mutations constitute a major mode of oncogenic activation of the Met receptor tyrosine kinase. Met is aberrantly activated in many types of human malignancies and its deregulated activity is correlated with aggressive tumor traits such as abnormal proliferation and
Martin Sattler et al.
Cancer research, 63(17), 5462-5469 (2003-09-23)
The Met receptor tyrosine kinase has been shown to be overexpressed or mutated in a variety of solid tumors and has, therefore, been identified as a good candidate for molecularly targeted therapy. Activation of the Met tyrosine kinase by the
Xueyan Wang et al.
Molecular cancer therapeutics, 2(11), 1085-1092 (2003-11-18)
The hepatocyte growth factor/scatter factor (HGF/SF) receptor, Met, mediates various cellular responses on activation with its ligand, including proliferation, survival, motility, invasion, and tubular morphogenesis. Met expression is frequently up-regulated in sarcomas and carcinomas. Experimental evidence suggests that Met activation
Patrick C Ma et al.
Cancer research, 65(4), 1479-1488 (2005-03-01)
Non-small cell lung cancer (NSCLC) is a difficult disease to treat. The c-Met receptor is an attractive potential target for novel therapeutic inhibition in human cancers. We provide strong evidence that c-Met is overexpressed, activated, and sometimes mutated in NSCLC
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