米非司酮 T1102

Product Introduction
Bioactivity


英文名: Mifepristone

描述: Mifepristone (C-1073) 是一种黄体酮受体和糖皮质激素受体拮抗剂，在体外实验中的 IC50值分别为 0.2 nM 和 2.6 nM。

细胞实验: 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)

激酶实验: 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.

体外活性: Mifepristone按最高剂量作用于大鼠,明显减少前列腺重量,且很大程度抑制二氢睾酮引起的前列腺的生长,且诱导萎缩和细胞死亡.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肿瘤生长.

体内活性: Mifepristone抑制人类肺癌细胞A549种皮质激素诱导的糖皮质激素反应元件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增殖,IC50分别为6.25 μM和6.91 μM。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 2.15 mg/mL (5 mM, suspension)
DMSO : 45 mg/mL (104.75 mM)
Ethanol : 21.5 mg/mL (50 mM))


关键字: 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

相关产品: AZD9977 | Beclometasone | Hydrocortisone 17-butyrate | Corticosterone | Fludrocortisone acetate | Canrenoate potassium | AL 082D06 | Beclometasone dipropionate | Drospirenone | Prednisone acetate

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Anti-Metabolism Disease Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Traditional Chinese Medicine Monomer Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途