| 中文名称: | 变棉子酚 | ||||
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| 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 | ||||
基本信息
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产品编号：A11308 |
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产品名称：(+)-Apogossypol |
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CAS: |
66389-74-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
494.60 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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生物活性
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产品描述 |
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。 |
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靶点/IC50 |
Mcl-1 2.6μM (EC50) |
Bcl-2 2.8μM (EC50) |
Bcl-xL 3.69μM (EC50) |
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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 1.7µM.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 9.57μM, while the IC50 of Gossypol on LNCaP cells is 10.35μM. |
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体内研究 |
Due to its modified structure, (+)-Apogossypol is expected to exhibit lower toxicity while maintaining the significant antigrowth 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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推荐实验方法(仅供参考)
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细胞实验: |
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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 10μM) and Gossypol are added into each well with gradient concentrations (2-20μM). For the cell viability test, tumor cells are suspended in a mixed solution of 200μL complete medium and 0.2μL DMSO, and wells with 200μL complete medium are used as blank controls. The plates are incubated at 37℃ with 5% CO2 for 72h. The medium is then removed, and 0.5μM MTT is added into the wells. After another 4h, 150μL DMSO is added into each well. The absorbance is read at 570nm on a microplate reader. The drug concentration yielding 50% cell inhibition (IC50) is determined. All experiments are performed in triplicate. |
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动物实验: |
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Mice Female athymic nude (nu/nu) mice (4-6 weeks of age, weighing 20-25g) 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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
