AZ 628

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Cat.No. 4836 - AZ 628 | C27H25N5O2 | CAS No. 878739-06-1
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
Literature

Biological Activity

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

AZ 628 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: AZ 628, supplier, AZ628, AZ_628, potent, Raf, kinases, inhibitors, inhibits, B-Raf, c-Raf, Raf, Kinase, Raf, Kinase, Tocris Bioscience

Citations for AZ 628

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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for AZ 628

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