AZ-628 is an irreversible Raf kinase inhibitor that exhibits anticancer chemotherapeutic activity in vitro and in vivo. AZ-628 strongly inhibits tumor cell growth in cells exhibiting mutant (V600E) B-Raf, a mutation commonly found in a variety of cancer subtypes; this compound also inhibits growth in several cell lines that were resistant to most other Raf inhibitors. AZ-628 exhibits similar inhibition of B-Raf and c-Raf in vitro but appears to be selective for B-Raf in vivo.
| Cas No. | 878739-06-1 |
|---|---|
| Purity | ≥96% |
| Formula | C27H25N5O2 |
| Formula Wt. | 451.52 |
| Chemical Name | 3-(2-cyanopropan-2-yl)-N-(4-methyl-3-(3-methyl-4-oxo-3,4-dihydroquinazolin-6-ylamino)phenyl)benzamide |
| IUPAC Name | 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl) amino]phenyl]benzamide |
| Solubility | DMSO 90 mg/mL (199.32 mM) Water Insoluble Ethanol Insoluble |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
|---|---|
| Info Sheet | |
| Brochures |
Whittaker SR, Theurillat JP, Van Allen E, et al. A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition. Cancer Discov. 2013 Mar;3(3):350-62. PMID: 23288408.
Montagut C, Sharma SV, Shioda T, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 2008 Jun 15;68(12):4853-61. PMID: 18559533.
