Home / Raf Kinase Inhibitors / AZ 628

AZ 628

Catalog #: 4836
2 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4836/10
4836/50
AZ 628 | CAS No. 878739-06-1 | Raf Kinase Inhibitors
1 Image
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%

Product Details
Citations (2)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
451.52
Formula:
C27H25N5O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
878739-06-1

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.

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

Background References

  1. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
    Hatzivassiliou et al.
    Nature, 2010;464:431
  2. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma.
    Montagut et al.
    Cancer Res., 2008;68:4853
  3. Selective Raf inhibition in cancer therapy.
    Khazak et al.
    Expert Opin.Ther.Targets, 2007;11:1587

Product Datasheets

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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

  1. 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
  2. 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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