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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1207993-83-6
- 分子式: C20H14Cl2N6O5S
- 分子量:521.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Cell Line
|
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
|
[PMID: 21126804] |
| MCF7 | IC50 |
0.355 μM
Compound: (RS)-14
|
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] |
化学情報
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CAS 番号 1207993-83-6
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分子量 521.33
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)