66389-74-0
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
| 熔点 | 118-123 °C |
| 沸点 | 673.3±50.0 °C(Predicted) |
| 密度 | 1.335±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | >16.2mg/mL in DMSO with gentle warming |
| 酸度系数(pKa) | 8.03±0.50(Predicted) |
| 形态 | 粉末 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
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).