AZ 628

Name: AZ 628
Brand: Tocris Bioscience
SKU: 4836

Tocris Bioscience a Bio-Techne Brand

Catalog # 4836

Citations (2)

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Key Product Details

Description:	Potent Raf kinase inhibitor
Chemical Name:	3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide
Purity:	≥98% (HPLC)
Molecular Weight:	451.52

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Biological Activity for AZ 628

AZ 628 is a potent, ATP-competitive inhibitor of Raf kinases (IC₅₀ values are 29, 34 and 105 nM for c-Raf1, B-Raf^V600E 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-Raf^V600E mutation.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Compound Libraries for AZ 628

AZ 628 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for AZ 628

M. Wt	451.52
Formula	C₂₇H₂₅N₅O₂
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	878739-06-1
PubChem ID	11676786
InChi Key	ZGBGPEDJXCYQPH-UHFFFAOYSA-N
Smiles	CC(C)(C#N)C1=CC=CC(C(NC2=CC(NC3=CC(C(N(C)C=N4)=O)=C4C=C3)=C(C)C=C2)=O)=C1

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.

Solubility for AZ 628

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	45.15	100

Preparing Stock Solutions for AZ 628

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

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References for AZ 628

References are publications that support the biological activity of the product.

Hatzivassiliou RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 2010 PMID: 20130576
Montagut Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 2008 PMID: 18559533
Khazak Selective Raf inhibition in cancer therapy. Expert Opin.Ther.Targets 2007 PMID: 18020980

Citations for AZ 628 (2)

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Citations are publications that use Bio-Techne products. Selected citations for AZ 628 include:

Echeverría et al. (2019) The sensitivity to Hsp90 inhibitors of both normal and oncogenically transformed cells is determined by the equilibrium between cellular quiescence and activity. PLoS One. 14:e0208287
PMID: 30726209
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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