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Description: AZ-628 (AZ628; AZ 628) is a novel, selective, and orally bioavailable Raf inhibitor with potential antineoplastic activity. It exhibits excellent pharmacokinetic properties and robust tumor growth inhibition in xenograft animal models. AZ-628 inhibits Raf isoforms such as c-Raf1, B-RafV600E and wild-type B-Raf with IC50 values of 29, 34 and 105 nM, respectively. AZ-628 potently inhibits the proliferation, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
References: Cancer Discov, 2013, 3(3):350-62.
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