c-Raf Inhibitor

General description

A cell-permeable pyrazoloimidazole phenyl urea derivative that acts as a selective type II inhibitor of c-Raf. It shows an IC₅₀ value of 50 nM in an enzymatic assay, and comparable anti-proliferative activities to sorafenib against A375P (GI ₅₀ = 2.68 µM) and WM3629 (GI₅₀ = 0.86 µM) human melanoma cell lines. When screening against a panel of 30 different kinases at a concentration of 10 µM, it exerts an inhibitory activity of 96% on c-Raf, but below 50% for most of the other kinases.

Legal Information

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

Other Notes

Yu, H., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3805.

Packaging

20 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)