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Merck
CN

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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关于此项目

经验公式（希尔记法）:
C28H30ClN5O4S
化学文摘社编号:
658084-23-2
分子量:
568.09
UNSPSC Code:
12352200
MDL number:
MFCD08276928

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产品名称

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.

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

assay

≥98% (HPLC)

form

powder
solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange

solubility

DMSO: 1 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes
Primary Target
met kinase activity
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM against Met kinase activity

Disclaimer

Toxicity: Irritant (B)

General description

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.

Other Notes

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.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warm as needed for complete solubilization.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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
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
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
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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