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Beschreibung

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 µ,M) and WM3629 (GI50 = 0.86 µ,M) human melanoma cell lines. When screening against a panel of 30 different kinases at a concentration of 10 µ,M, it exerts an inhibitory activity of 96% on c-Raf, but below 50% for most of the other kinases.