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Metabolism GR Mifepristone

Mifepristone

Catalog No. T1102   CAS 84371-65-3
Synonyms: RU 38486, RU486, C-1073
Purity 99.76% Datasheet MSDS

Mifepristone is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Mifepristone, CAS 84371-65-3
Pack Size Availability Price/USD Quantity
5 mg In stock 25.00
10 mg In stock 30.00
50 mg In stock 38.00
100 mg In stock 55.00
200 mg In stock 80.00
500 mg Inquiry 100.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Mifepristone is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.
Targets&IC50 Glucocorticoid Receptor :ic50 2.6nM,   PR :ic50 0.2nM,  
Kinase Assay 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 Research
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)
Cell lines: OV2008 and SK-OV-3 cells
Animal Research
Animal Model: SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice.

Description

Mifepristone is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Targets&IC50

Glucocorticoid Receptor :ic50 2.6nM

PR :ic50 0.2nM

In Vitro

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。

In Vivo

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。

Kinase Assay

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 Research

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)

Cell lines: OV2008 and SK-OV-3 cells

Animal Research

Animal Model: SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice.

Synonyms RU 38486, RU486, C-1073
Purity 99.76%
Appearance solid
Molecular Weight 429.60
Formula C29H35NO2
CAS No. 84371-65-3

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 43 mg/mL (100 mM)

Ethanol: 21.5 mg/mL (50 mM), with gentle warming

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Jiang W, et al. Bioorg Med Chem, 2006, 14(19), 6726-6732. 2. Goyeneche AA, et al. Clin Cancer Res, 2007, 13(11), 3370-3379. 3. Wang Y, et al. Stem Cells, 2012, 30(2), 169-179. 4. Cabeza M, et al. J Steroid Biochem Mol Biol, 2007, 104(3-5), 321-325.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Autophagy Compound Library Endocrinology-Hormones Library FDA-approved Drug Library GPCR Compound Library Anti-Metabolism Disease Compound Library

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