apogossypol Chemical Properties

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)

apogossypol Usage And Synthesis

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

IC 50

Mcl-1: 2.6 μM (EC₅₀); Bcl-2: 2.8 μM (EC₅₀); Bcl-xL: 3.69 μM (EC₅₀)

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