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(+)-Apogossypol

CAS No. : 66389⁻⁷4-0

MCE 国际站：(+)-Apogossypol

产品活性：(+)-Apogossypol 是一种泛 BCL-2 拮抗剂，与 Mcl-1, Bcl-2 和 Bcl-xL 结合， EC₅₀ 分别为 2.6，2.8 和 3.69 µM。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

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.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.

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. 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).

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