Met Kinase Inhibitor VI, SGX523-CAS 1022150-57-7-Calbiochem

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一般描述

A cell-permeable triazolopyridazine compound that acts as a potent, ATP-competitive (K_i= 2.7 & 23 nM using non-phosphorylated and phosphorylated MET kinase domain, respectively), and highly selective inhibitor against the tyrosine kinase activity of the HGF (hepatocyte growth factor) receptor c-MET (IC₅₀= 4 nM), while exhibiting little or no activity toward a panel of more than 210 other kinases, including the closely related RTK RON. Shown to inhibit the constitutive (IC₅₀= 40 nM in GTL16 cells) as well as HGF-stimulated (IC₅₀= 12 nM in A549 cells) MET autophosphorylation/activation in culturesin vitroand effectively suppress MET-dependent tumor growths in micein vivo(twice daily oral dosings at 30 mg/kg). X-ray crystallography reveals that SGX523 locks MET in a "DFG-in" conformation with the triazolopyridazine moiety interacting with the hydrophobic side chains of Met¹²²⁹and Tyr¹²⁴⁸, while Tyr¹²⁴⁸mutations are found to render MET insensitive to SGX523 inhibition both in cell-free and cell-based assays.

包装

5 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C.

其他说明

Buchanan, S.G., et al. 2009.Mol. Cancer Ther.8,3181.
Eder, J.P., et al. 2009.Clin. Cancer Res.15,2207.

法律信息

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

基本信息

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