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AZ-628 | Raf inhibitor

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Price:
$159.00
Catalog #:
C2962-5
Quantity:


Product Description

AZ628 is a quinazolinone-based pan-Raf kinase inhibitor with IC50 values of 105, 34, and 29 nM for b-Raf, bRafV600E, and c-Raf-1, respectively. [1] It is selective over a wide panel of RTKs, including VEGFR2, DDR2, Lyn, Flt1, and FMS. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines with the b-RafV600E mutation. Cross-reactivity profiles of AZ628 indicate similarities to sorafenib.

Typically AZ628-sensitive lines are often characterized by b-RAFV600E or NRAS mutations, while HRAS or KRAS mutations were not normally observed. AZ628 sensitivity is correlates with its abaility to suppress downstream ERK. [2]


Technical information:

Chemical Formula:   C27H25N5O2
CAS #:   878739-06-1
Molecular Weight:   451.52
Purity:   > 99%
Appearance:   White
Chemical Name:   3-(2-cyanopropan-2-yl)-N-(4-methyl-3-(3-methyl-4-oxo-3,4-dihydroquinazolin-6-ylamino)phenyl)benzamide
Solubility:   Up to 22 mM in DMSO
Synonyms:   AZ-628, AZ 628, AZ628

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Khazak et al., Selective Raf inhibition in cancer therapy. Expert Opin. Ther. Targets, 2007, 11(12), 1587-1609. Pubmed ID: 18020980
2. McDermott et al., Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc. Natl. Acad. Sci. 104(50), 19936-19941. Pubmed ID: 18077425

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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