Biochem/physiol Actions

Target IC₅₀: 20 nM against Met kinase activity

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Primary Targetmet kinase activity

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.

Legal Information

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

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

1 mg in Plastic ampoule

Packaged under inert gas

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.

Warning

Toxicity: Irritant (B)