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448101

Sigma-Aldrich

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.

Synonym(s):

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

Empirical Formula (Hill Notation):
C28H30ClN5O4S
CAS Number:
658084-23-2
Molecular Weight:
568.09
MDL number:
MFCD08276928
UNSPSC Code:
12352200

Quality Level

100

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

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

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.

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Preparation Note

Warm as needed for complete solubilization.

Reconstitution

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

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.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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
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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