1207993-83-6
Chemical Structure
Bozepinib
- CAS No.: 1207993-83-6
- Formula:C20H14Cl2N6O5S
- Molecular Weight:521.33
IUPAC Name: 3-(2,6-dichloro-9H-purin-9-yl)-1-((4-nitrophenyl)sulfonyl)-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepine
InChIKey: ADWZQHLAYGEBHB-UHFFFAOYSA-N
SMILES: O=S(N1CC(OCC2=CC=CC=C21)N3C=NC4=C3N=C(N=C4Cl)Cl)(C5=CC=C(C=C5)[N+]([O-])=O)=O
Biological Activity: 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].
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Bozepinib | 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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
