Potent, 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
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.
Sold with the permission of AstraZeneca UK Ltd.
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
Hatzivassiliou et al.
Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma.
Montagut et al.
Cancer Res., 2008;68:4853
Selective Raf inhibition in cancer therapy.
Khazak et al.
Expert Opin.Ther.Targets, 2007;11:1587