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.
For research use only. We do not sell to patients.
- CAS No.: 1207993-83-6
- Formula: C20H14Cl2N6O5S
- Molecular Weight:521.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
1.825 μM
Compound: (RS)-14
|
Cytotoxicity against human MCF10A cells after 3 days by SRB assay
Cytotoxicity against human MCF10A cells after 3 days by SRB assay
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[PMID: 21126804] |
| MCF7 | IC50 |
0.355 μM
Compound: (RS)-14
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Cytotoxicity against human MCF7 cells expressing wild type p53 and ras mutant after 3 days by SRB assay
Cytotoxicity against human MCF7 cells expressing wild type p53 and ras mutant after 3 days by SRB assay
|
[PMID: 21126804] |
| MDA-MB-231 | IC50 |
0.166 μM
Compound: (RS)-14
|
Cytotoxicity against human MDA-MB-231 cells expressing high level of p53 after 3 days by SRB assay
Cytotoxicity against human MDA-MB-231 cells expressing high level of p53 after 3 days by SRB assay
|
[PMID: 21126804] |
Chemical Information
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CAS No. 1207993-83-6
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Molecular Weight 521.33
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Formula C20H14Cl2N6O5S
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SMILES
O=S(N1CC(OCC2=CC=CC=C21)N3C=NC4=C3N=C(N=C4Cl)Cl)(C5=CC=C(C=C5)[N+]([O-])=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)