| Identification | Back Directory | [Name]
apogossypol | [CAS]
66389-74-0 | [Synonyms]
NSC736630
apogossypol
(+)-APOGOSSYPOL
APOGOSSYPOL;NSC736630
(+)-3,3'-Dimethyl-5,5'-bis(1-methylethyl)-2,2'-binaphthalene-1,1',6,6',7,7'-hexol
[2,2'-Binaphthalene]-1,1',6,6',7,7'-hexol, 3,3'-dimethyl-5,5'-bis(1-methylethyl)-, (2S)-
3-methyl-5-propan-2-yl-2-(1,6,7-trihydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)naphthalene-1,6,7-triol | [Molecular Formula]
C28H30O6 | [MOL File]
66389-74-0.mol | [Molecular Weight]
462.53 |
| Chemical Properties | Back Directory | [Melting point ]
118-123 °C | [Boiling point ]
673.3±50.0 °C(Predicted) | [density ]
1.335±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
>16.2mg/mL in DMSO with gentle warming | [form ]
Powder | [pka]
8.03±0.50(Predicted) |
| Hazard Information | Back Directory | [Uses]
(+)-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. | [Biological Activity]
(+)-Apogossypol is a pan-BCL-2 antagonist that binds to Mcl-1, Bcl-2 and Bcl-xL with EC50 of 2.6, 2.8 and 3.69 μM, respectively. | [in vitro]
In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with K d values of 1.7 μM. | [in vivo]
Due to its modified structure, (+)-Apogossypol is expected to exhibit lower toxicity while maintaining the significant anti-growth and anti-tumor activities in vitro, similar to those of Gossypol. | [target]
| Mcl-1 < span> 2.6 μM (EC 50 ) | Bcl-2 2.8 μM (EC 50 ) | Bcl-xL 3.69 μM (EC 50 ) | | [IC 50]
Mcl-1: 2.6 μM (EC50); Bcl-2: 2.8 μM (EC50); Bcl-xL: 3.69 μM (EC50) | [storage]
Store at -20°C | [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. DOI:10.1158/1535-7163.MCT-08-1050
[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. DOI:10.3892/mmr.2015.3326 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|