Mifepristone
(Synonyms: 米非司酮; RU486; RU 38486) 目录号 : GC11637A glucocorticoid, progesterone, and androgen receptor antagonist
Cas No.:84371-65-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment [1]: | |
Glucocorticoid receptor (GR) antagonist activity, Progesterone receptor (PR) antagonist activity |
T47D alkaline phosphatase assay: T47D human breast cancer cells are plated in 96-well tissue culture plates at 104 cells per well in assay medium [RPMI medium without phenol red containing 5% (v/v) charcoal-treated FBS and 1% (v/v) penicillin–streptomycin]. Two days later, the medium is decanted and Mifepristone or control is added at a final concentration of 0.1% (v/v) dimethylsulfoxide in fresh assay medium. Twenty-four hours later, an alkaline phosphatase assay is performed using a SEAP kit. The medium is decanted and the cells are fixed for 30 minutes at room temperature with 5% (v/v) formalin. The cells are washed once at room temperature with Hanks' buffered saline solution. Equal volumes (0.05 mL) of dilution buffer, assay buffer, and 1:20 substrate/enhancer mixture are then added. After 1-hour incubation in the dark at room temperature, the lysate is transferred to a white 96-well plate and luminescence is read using a LuminoSkan Ascen. A549 reporter assay: A549 human lung carcinoma cells are washed with OPTI-MEM I. The medium is removed and lipid–DNA complex solution (1.5 μg/mL of GRE-luciferase reporter DNA in 8.5 mL OPTI-MEM I plus 6 μL/mL DMRIE-C reagent in 8.5 mL OPTI-MEM I, combined, mixed and incubated at room temperature for 40 minutes) is overlayed onto the cells in a T160 flask. The cells are incubated for 16 hours at 37 °C in a CO2 incubator. The DNA-containing medium is removed and 30 mL of growth medium containing 5% (v/v) charcoal-treated fetal bovine serum is added. After 5-6 hours, the cells are seeded in 96-well plates and incubated overnight at 37 °C. Mifepristone is then added to each well followed by dexamethasone as a corticoid challenge. The cells are incubated for 24 hours. Luciferase assay buffer is added to each well and the cells are incubated for 30 minutes at room temperature. Luciferase activity is measured in a DYNEX Microlite plate on a TopCount. |
Cell experiment: | |
Cell lines |
Sperm; ovarian cancer cell lines(SK-OV-3, Caov-3, IGROV-1, and OV2008 cells) |
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
0.04, 0.4, 4 and 40 μM for 1 h; or 20 μM for 1-3 days |
Applications |
Mifepristone modulated human sperm functions and dose-dependently inhibited progesterone-induced acrosome reaction, hyperactivation and [Ca2+]i in human spermatozoa [2]. Moreover, mifepristone suppressed cell growth and decreased the expression of the S phase cyclin (cyclin A) and the M phase cyclin (cyclin B1) in various ovarian cancer cell lines [3]. |
Animal experiment: | |
Animal models |
SK-OV-3 tumor xenografts model |
Dosage form |
0.5, 1.0 mg/d, s.c., for 40 days |
Applications |
Mifepristone (0.5, 1.0 mg/d) dose-dependently inhibited SK-OV-3 tumors growth in nude mice [3]. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: 1. Jiang, W., Allan, G., Fiordeliso, J. J., Linton, O., Tannenbaum, P., Xu, J., Zhu, P., Gunnet, J., Demarest, K., Lundeen, S. and Sui, Z. (2006) New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids. Bioorg Med Chem. 14, 6726-6732 2. Ko, J. K., Huang, V. W., Li, R. H., Yeung, W. S., Ho, P. C. and Chiu, P. C. (2014) An in vitro study of the effect of mifepristone and ulipristal acetate on human sperm functions. Andrology. 2, 868-874 3. Goyeneche, A. A., Caron, R. W. and Telleria, C. M. (2007) Mifepristone inhibits ovarian cancer cell growth in vitro and in vivo. Clin Cancer Res. 13, 3370-3379 |
Mifepristone (RU486) is a potent antagonist of progesterone receptor, used as a contraceptive agent [1].
As a contraceptive agent, Mifepristone has been reported to reduce the size of uterine fibroids, and inhibit the growth of meningioma cells in vitro, in experimental animal models and in patients with inoperable meningiomas. As a non-contraceptive action, Mifepristone was been revealed to inhibit the proliferation of normal and malignant endometrial cells, breast cancer cells, prostate cancer cells and gastric adenocarcinoma cell lines. In addition, Mifepristone has been demonstrated to have progesterone-like effects and suppression ovarian cancer cell growth in a dose-dependent fashion with the IC50 values of 6.25μmol/l and 6.91μmol/l for SK-OV-3 and OV2008 cell lines, respectively [1].
References:
[1] Goyeneche AA1, Carón RW, Telleria CM. Mifepristone inhibits ovarian cancer cell growth in vitro and in vivo. Clin Cancer Res. 2007 Jun 1; 13(11):3370-9.
Cas No. | 84371-65-3 | SDF | |
别名 | 米非司酮; RU486; RU 38486 | ||
化学名 | (8S,11R,13S,14S,17S)-11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one | ||
Canonical SMILES | CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O | ||
分子式 | C29H35NO2 | 分子量 | 429.59 |
溶解度 | ≥ 21.4795 mg/mL in DMSO, ≥ 21.45 mg/mL in EtOH with gentle warming | 储存条件 | Store at 2-8°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 | |||
1 mg | 5 mg | 10 mg | |
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
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 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% 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,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。