Cat. No. Name Size Price Add Cart
KI2358AZ6285 mg$240
AZ62825 mg$752

Chemical Characteristic

Product NameAZ628
SynonymsN/A
CAS No.878739-06-1
Molecular Weight 451.52
FormulaC27H25N5O2
Chemical Name3-(2-cyanopropan-2-yl)-N-(4-methyl-3-(3-methyl-4-oxo-3,4-dihydroquinazolin-6-ylamino)phenyl)benzamide
SmilesC(=O)(c1cc(ccc1)C(C)(C)C#N)Nc1cc(c(cc1)C)Nc1cc2c(=O)n(cnc2cc1)C
Chemical Structure

Biological activities

AZ628 is a selective BRAF inhibitor. AZ628 inhibits WT BRAF and mutant BRAF with IC50s of 2.14 mM and 196 nM, respectively.[1] AZ628 inhibits BRAF V600E, wild-type CRAF, and wild-type BRAF with IC50s of 30, 30 and 100 nM, respectively. AZ628 effectively inhibits the growth of a specific subset of human cancer cell lines derived from melanomas, thyroid cancers, and colorectal cancers.[2]

Protocols

In vitro, AZ628 is dissolved DMSO.[3]

References

[1] McDermott U, et al. Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007, 104(50): 19936-19941.
[2] Montagut C, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 2008, 68(12): 4853-4861.
[3] Corcoran RB, et al. BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutation. Sci Signal. 2010, 3(149): ra84.

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