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.
Sold with the permission of AstraZeneca UK Ltd.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 451.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.21 mL||11.07 mL||22.15 mL|
|5 mM||0.44 mL||2.21 mL||4.43 mL|
|10 mM||0.22 mL||1.11 mL||2.21 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for AZ 628, please let us know.
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Keywords: AZ 628, AZ 628 supplier, AZ628, AZ_628, potent, Raf, kinases, inhibitors, inhibits, B-Raf, c-Raf, Kinase, 4836, Tocris Bioscience
1 Citation for AZ 628
Citations are publications that use Tocris products. Selected citations for AZ 628 include:
Sahu et al (2016) Functional screening implicates miR-371-3p and peroxiredoxin 6 in reversible tolerance to cancer drugs. Nat Commun 7 12351 PMID: 27484502
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Literature in this Area
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