66389-74-0
66389-74-0 结构式
基本信息
变棉子酚
阿朴棉子酚
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
物理化学性质
常见问题列表
|
Mcl-1 2.6 μM (EC 50 ) |
Bcl-2 2.8 μM (EC 50 ) |
Bcl-xL 3.69 μM (EC 50 ) |
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.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 (IC 50 ) on LNCaP cells within ~72 h is 9.57 μM, while the IC 50 of Gossypol on LNCaP cells is 10.35 μM.
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. The anti-cancer effect of (+)-Apogossypol is evaluated in mice bearing subcutaneous LNCaP cell xenografts. The tumor growth is monitored and measured by a caliper and balance. The survival rate of the mice is notably improved by (+)-Apogossypol. Of note, the tumor sizes are also markedly decreased by (+)-Apogossypol treatment (P<0.01).