(+)-Apogossypol
(+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 66389-74-0
- Formula: C28H32O6
- Molecular Weight:462.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Mcl-1 2.6 μM (EC50) |
Bcl-2 2.8 μM (EC50) |
Bcl-xL 3.69 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| NCI-H1299 | EC50 |
3.4 μM
Compound: 2, Apogossypol
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Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
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[PMID: 19555126] |
| NCI-H460 | EC50 |
3.5 μM
Compound: 2, Apogossypol
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Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
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[PMID: 19555126] |
In Vitro
In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with Kd values of 1.7 µM[1].To investigate the inhibitory effects of (+)-Apogossypol and Gossypol on LNCaP cell survival, the MTT assay is performed. The results demonstrate that (+)-Apogossypol inhibits the proliferation of LNCaP cells in a time- and dose-dependent manner, in a similar way with Gossypol. The concentration for 50% inhibition (IC50) on LNCaP cells within ~72 h is 9.57 μM, while the IC50 of Gossypol on LNCaP cells is 10.35 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 66389-74-0
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Molecular Weight 462.54
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Formula C28H32O6
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SMILES
OC1=C2C=C(O)C(O)=C(C(C)C)C2=CC(C)=[C@@]1[C@@]3=C(C)C=C4C(C(C)C)=C(O)C(O)=CC4=C3O
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Synonyms
Apogossypol; NSC736630
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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]. Wei J, et al. Apogossypol derivatives as antagonists of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2009 Apr;8(4):904-13. [Content Brief]
[2]. Zhan W, et al. Inhibitory activity of apogossypol in human prostate cancer in vitro and in vivo. Mol Med Rep. 2015 Jun;11(6):4142-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(+)-Apogossypol Related Classifications
HY-13408 Related Classifications
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