Cat. No. 4836
Chemical Name: 3-(1-Cyano-1-methylethyl)-N-[3-[(3,
Biological ActivityPotent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM for c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity for Raf kinases over a panel of 150 other kinases; inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. Also inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
Licensing InformationSold with the permission of AstraZeneca UK Ltd.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Hatzivassiliou et al (2010) RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464 431. PMID: 20130576.
Montagut et al (2008) Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 68 4853. PMID: 18559533.
Khazak et al (2007) Selective Raf inhibition in cancer therapy. Expert Opin.Ther.Targets 11 1587. PMID: 18020980.
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Keywords: AZ 628, supplier, AZ628, AZ_628, potent, Raf, kinases, inhibitors, inhibits, B-Raf, c-Raf, Tocris Bioscience, Raf Kinase Inhibitor products
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