| Identification | Back Directory | [Name]
Bozepinib | [CAS]
1207993-83-6 | [Synonyms]
Bozepinib
4,1-Benzoxazepine, 3-(2,6-dichloro-9H-purin-9-yl)-1,2,3,5-tetrahydro-1-[(4-nitrophenyl)sulfonyl]- | [Molecular Formula]
C20H14Cl2N6O5S | [MOL File]
1207993-83-6.mol | [Molecular Weight]
521.33 |
| Hazard Information | Back Directory | [Uses]
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice[1][2]. | [Enzyme inhibitor]
This potent antitumor agent (FW = 521.33 g/mol), sysyematically known as (RS)-2,6-dichloro-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1- benzoxazepin-3-yl]-9H-purine, induces apoptosis in breast and colon cancer cells via inhibition (IC50 = 0.3–2 μM) of the the double-stranded RNAdependent protein kinase, PKR, but not p53. Moreover, interferon enhances cytotoxicity of bozepinib in colon and breast cancer cells by increasing apoptotic cell death. | [References]
[1] Marchal JA, et al. Bozepinib, a novel small antitumor agent, induces PKR-mediated apoptosis and synergizes with IFNα triggering apoptosis, autophagy and senescence. Drug Des Devel Ther. 2013 Oct 29;7:1301-13. DOI:10.2147/DDDT.S51354
[2] Ramírez A, et al. HER2-signaling pathway, JNK and ERKs kinases, and cancer stem-like cells are targets of Bozepinib small compound. Oncotarget. 2014 Jun 15;5(11):3590-606. DOI:10.18632/oncotarget.1962 |
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