| 名稱 | Mifepristone |
| 描述 | Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist. |
| 細(xì)胞實(shí)驗(yàn) | Cell growth is evaluated in various ovarian cancer cell lines that are subjected to dose-response or time course treatments. Media containing each of the doses of fresh steroids is replaced every 24 hours. Control groups of cells are treated with vehicle ethanol at a final concentration of less than 0.05%. Number of viable cells is evaluated by trypsinization and counting in a hemocytometer chamber using trypan blue dye exclusion. Experiments are conducted in 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, all subsequent experiments are conducted using media with unextracted serum and in the presence of phenol red. When indicated, the proliferation IC50s are calculated using software designed to study drug interaction. (Only for Reference) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | Mifepristone抑制人類肺癌細(xì)胞A549種皮質(zhì)激素誘導(dǎo)的糖皮質(zhì)激素反應(yīng)元件偶聯(lián)的熒光素酶報(bào)告基因轉(zhuǎn)錄。而且,Mifepristone作用于人類乳腺癌細(xì)胞T47D,也阻斷孕酮對(duì)堿性磷酸酶活性的誘導(dǎo)作用。Mifepristone抑制卵巢癌細(xì)胞SK-OV-3 和OV2008增殖,IC50分別為6.25 μM和6.91 μM。 |
| 體內(nèi)活性 | Mifepristone按最高劑量作用于大鼠,明顯減少前列腺重量,且很大程度抑制二氫睪酮引起的前列腺的生長,且誘導(dǎo)萎縮和細(xì)胞死亡.每天0.5 mg和1 mg Mifepristone作用于免疫抑制小鼠,可以抑制SK-OV-3腫瘤生長. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.3 mg/mL (10.01 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 45 mg/mL (104.75 mM)
Ethanol : 21.5 mg/mL (50 mM)), Heating is recommended.
|
| 關(guān)鍵字 | Mifepristone | RU38486 | Inhibitor | RU-38486 | NOS | NO Synthase | Nitric oxide synthases | NR3C3 | Glucocorticoid Receptor | Autophagy | inhibit | C1073 | RU-486 | C 1073 | Progesterone Receptor | RU 486 |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 抑制劑庫 | 神經(jīng)保護(hù)化合物庫 | 抗癌上市藥物庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |