中文名称: | 变棉子酚 | ||||
---|---|---|---|---|---|
英文名称: | (+)-Apogossypol | ||||
别名: | 變棉子酚;阿朴棉子酚 Apogossypol; NSC736630 | ||||
CAS No: | 66389-74-0 | 分子式: | C28H30O6S | 分子量: | 494.6 |
CAS No: | 66389-74-0 | ||||
分子式: | C28H30O6S | ||||
分子量: | 494.6 |
包装规格:
25mg 50mg 100mg 250mg 500mg in glass bottle
产品简介:
一种泛 BCL-2 拮抗剂,与 Mcl-1, Bcl-2 和 Bcl-xL 结合, EC50 分别为 2.6,2.8 和 3.69μM。
靶点:
Mcl-1:2.6 μM (EC50);Bcl-2:2.8 μM (EC50);Bcl-xL:3.69 μM (EC50)
体外研究:
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.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.
体内研究:
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).
保存条件:
-20℃
注意事项:
1、为了您的安全和健康,请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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稀释公式
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