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(+)-Apogossypol (Synonyms: Apogossypol; NSC736630)
(+)-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。
(+)-Apogossypol Chemical Structure
CAS No. : 66389-74-0
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生物活性 |
(+)-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. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
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[1].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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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)[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
462.54 |
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Formula |
C28H32O6 |
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CAS 号 |
66389-74-0 |
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中文名称 |
變棉子酚;阿朴棉子酚;变棉子酚 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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Cell Assay [2] |
The cytotoxic effect of (+)-Apogossypol and Gossypol on prostate cancer cell lines is measured by the MTT assay. LNCaP cells are seeded onto sterile 96 well flat bottomed plates and incubated overnight. Then diluted (+)-Apogossypol (1 and 10 μM) and Gossypol are added into each well with gradient concentrations (2-20 μM). For the cell viability test, tumor cells are suspended in a mixed solution of 200 μL complete medium and 0.2 μL DMSO, and wells with 200 μL complete medium are used as blank controls. The plates are incubated at 37°C with 5% CO2 for 72 h. The medium is then removed, and 0.5 μM MTT is added into the wells. After another 4 h, 150 μL DMSO is added into each well. The absorbance is read at 570 nm on a microplate reader. The drug concentration yielding 50% cell inhibition (IC50) is determined. All experiments are performed in triplicate[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
Mice[2] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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