生物活性
Mifepristone是一种异常活跃的孕激素受体和糖皮质激素受体拮抗剂,IC50分别为0.2nM和2.6 nM。Mifepristone 作用于人类肺癌细胞A549,抑制皮质激素诱导的糖皮质激素反应元件(GRE)偶联的荧光素酶报告基因转录。而且, Mifepristone作用于人类乳腺癌细胞T47D,也阻断孕酮对碱性磷酸酶活性的诱导作用。 Mifepristone抑制卵巢癌细胞SK-OV-3 和 OV2008生长,IC50分别为 6.25 μM 和 6.91 μM。
化学数据
分子量 | 429.59 |
分子式 | C29H35NO2 |
CAS号 | 84371-65-3 |
纯度 | 99.91% |
溶解性(25°C) | DMSO 76 mg/mL |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | OV2008 and SK-OV-3 cells |
方法 | Evaluating cell growth in various ovarian cancer cell lines that are subjected to dose-response or time course treatments.Replacing media containing each of the doses of fresh steroids every 24 hours. Treating control groups of cells with vehicle ethanol at a final concentration of less than 0.05%. Evluateing number of viable cells by trypsinization and counting in a hemocytometer chamber using trypan blue dye exclusion. Conducting experimentsin media without phenol red and supplemented with charcoal extracted fetal bovine serum, or media containing unextracted serum and having phenol red. Similar results are obtained with both media preparations; therefore, after performing the growth curves, using media with unextracted serum to conduct all subsequent experiments and in the presence of phenol red. When indicated, using software designed to study drug interaction to calculate the proliferation IC50s . |
浓度 | 0-20 μM |
处理时间 | 24 hours |
动物实验 |
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动物模型 | SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice. |
配制 | Constant release pellets (Innovative Research of America) |
剂量 | 0.5 or 1 mg/day |
给药处理 | Implanted s.c. with pellets |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.3278 mL | 11.639 mL | 23.278 mL |
5 mM | 0.4656 mL | 2.3278 mL | 4.6556 mL |
10 mM | 0.2328 mL | 1.1639 mL | 2.3278 mL |