Chemical Name: 3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide
Biological ActivityAZ 628 is a 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 mutation.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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
Citations for AZ 628
The citations listed below are publications that use Tocris products. Selected citations for AZ 628 include:
2 Citations: Showing 1 - 2
The sensitivity to Hsp90 inhibitors of both normal and oncogenically transformed cells is determined by the equilibrium between cellular quiescence and activity.
Authors: Echeverría Et al.
PLoS One 2019;14:e0208287
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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