Chemical Name: 3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide
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.
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.
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
Citation for AZ 628
The citations listed below are publications that use Tocris products. Selected citations for AZ 628 include:
1 Citation: Showing 1 - 1
Functional screening implicates miR-371-3p and peroxiredoxin 6 in reversible tolerance to cancer drugs.
Authors: Sahu Et al.
Nat Commun 2016;7:12351
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