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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.

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C28H30ClN5O4S
Numero CAS:
658084-23-2
Peso molecolare:
568.09
Numero MDL:
MFCD08276928
Codice UNSPSC:
12352200

Livello qualitativo

100

Saggio

≥98% (HPLC)

Stato

powder
solid

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

OK to freeze
protect from light

Colore

orange

Solubilità

DMSO: 1 mg/mL

Condizioni di spedizione

ambient

Temperatura di conservazione

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-
FPYJSJDOHRDAMT-KQWNVCNZSA-N

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Nota sulla preparazione

Warm as needed for complete solubilization.

Ricostituzione

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

Altre note

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.

Note legali

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

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘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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