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.

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

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

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Toxicity: Standard Handling (A)