AZ 628

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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)
Datasheet
Citations (2)
Reviews

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-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.

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 Data for AZ 628

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 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

2 Citations for AZ 628

Citations are publications that use Tocris 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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