The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer. BAY-43-9006 is an inhibitor of Raf-1 and B-Raf (IC50 = 6 and 22 nM, respectively), as well as several receptor tyrosine kinases, including vascular endothelial growth factor receptors 2 and 3, platelet-derived growth factor receptor β, Flt-3, and c-KIT (IC50 = 90, 15, 20, 57, and 58 nM, respectively). It poorly inhibits ERK-1, MEK-1, and several other kinases (IC50 >10 μM). Through these effects BAY-43-9006 inhibits tumor angiogenesis and induces tumor cell apoptosis, particularly in renal cell carcinoma and hepatocellular carcinoma.
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