(+)-Apogossypol
(Synonyms: 變棉子酚,Apogossypol; NSC736630) 目录号 : GC17008
(+)-Apogossypol 是一种泛 BCL-2 拮抗剂。 (+)-Apogossypol 与 Mcl-1、Bcl-2 和 Bcl-xL 结合，EC50 分别为 2.6、2.8 和 3.69 μM。
Cas No.:66389-74-0
Sample solution is provided at 25 µL, 10mM.
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(+)-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.
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].
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].
References:
[1]. Wei J, et al. Apogossypol derivatives as antagonists of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2009 Apr;8(4):904-13.
[2]. Zhan W, et al. Inhibitory activity of apogossypol in human prostate cancer in vitro and in vivo. Mol Med Rep. 2015 Jun;11(6):4142-8.
Cell experiment: | 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]. |
Animal experiment: | Mice[2]Female athymic nude (nu/nu) mice (4-6 weeks of age, weighing 20-25 g) are used. LNCaP cells (2×106) are injected subcutaneously into each mouse. The tumor volume is measured every two days using a caliper and calculated. When subcutaneous tumor sizes reach 150-200 mm3, these mice are randomly divided into three groups, each group consisting of 10 mice. Next, they are treated with (+)-Apogossypol and Gossypol, respectively, at 20 mg/kg intraperitoneally, q.d. every 7 d for 28 d. The vehicle control group receive the same amount of DMSO as in the treatment groups. The tumor volume is detected every day. The tumor tissues are fixed in 10% formalin solution. The tissues are embedded with paraffin, and the sections are prepared. Samples are stained with hematoxylin and eosin and microscopically examined. |
References: [1]. Wei J, et al. Apogossypol derivatives as antagonists of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2009 Apr;8(4):904-13. | |
| Cas No. | 66389-74-0 | SDF | |
| 别名 | 變棉子酚,Apogossypol; NSC736630 | ||
| 化学名 | (R)-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-1,1',6,6',7,7'-hexaol | ||
| Canonical SMILES | CC(C=C1C(C(C)C)=C(O)C(O)=CC1=C2O)=[C@]2[C@@]3=C(C)C=C4C(C=C(O)C(O)=C4C(C)C)=C3O | ||
| 分子式 | C28H30O6 | 分子量 | 462.53 |
| 溶解度 | ≥ 16.2mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.162 mL | 10.8101 mL | 21.6202 mL |
| 5 mM | 0.4324 mL | 2.162 mL | 4.324 mL |
| 10 mM | 0.2162 mL | 1.081 mL | 2.162 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >98.00%
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