(+)-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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
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Data Sheet (277 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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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