For research use only.
Catalog No.S2606 Synonyms: C-1073, RU 38486, Mifegyne
CAS No. 84371-65-3
Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Selleck's Mifepristone (RU486) has been cited by 14 publications
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Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.
PLoS One 2014 9(8), e105528. Mifepristone (RU486) purchased from Selleck.
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|Description||Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.|
|Features||Mifepristone is the first approved medication for patients with endogenous cushing|
Mifepristone inhibit corticoid-induced transcription from a glucocorticoid response element (GRE)-linked luciferase reporter gene in the human lung carcinoma cell line A549. Moreover, Mifepristone also blocks progesterone induction of alkaline phosphatase activity in the human breast cancer cell line T47D.  Mifepristone inhibits ovarian cancer cell growth of SK-OV-3 and OV2008 with IC50 of 6.25 μM and 6.91 μM, respectively.  A recent study shows that Mifepristone induces caspase-1 over expression both in differentiated and undifferentiated caspase-1-embryonic stem cells. 
Mifepristone can impair the growth of SK-OV-3 tumors in immunosuppressed mice at 0.5 mg/day and 1 mg/day.  Mifepristone inhibits the prostate weight significantly in the highest doses in vivo, and inhibits growth of the prostate gland produced by dihydrotestosterone (DHT) to a greater extent than the induction of atrophy and cell death in rats. 
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
-  Jiang W, et al. Bioorg Med Chem, 2006, 14(19), 6726-6732.
-  Goyeneche AA, et al. Clin Cancer Res, 2007, 13(11), 3370-3379.
-  Wang Y, et al. Stem Cells, 2012, 30(2), 169-179.
|In vitro||DMSO||85 mg/mL (197.86 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||C-1073, RU 38486, Mifegyne|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03258372||Completed||Drug: Mifepristone||Healthy||Corcept Therapeutics||August 16 2017||Phase 1|
|NCT03259542||Completed||Drug: Mifepristone 300 MG|Drug: Itraconazole 100 MG||Drug Interaction Potentiation|Healthy||Corcept Therapeutics||August 9 2017||Phase 1|
|NCT02720991||Completed||Drug: Mifepristone|Drug: Sublingual misoprostol||Abortion 3 Months||Gynuity Health Projects|Hopital La Rabta||July 2014||Phase 4|
|NCT02014337||Completed||Drug: Mifepristone and Eribulin in combination||Breast Cancer|Ovarian Epithelial Cancer Recurrent|Sarcoma|Non-small Cell Lung Cancer|Carcinoma Transitional Cell|Prostate Cancer|Prostatic Neoplasms||Corcept Therapeutics||January 2014||Phase 1|
|NCT01811056||Completed||Drug: Mifepristone||Termination of Pregnancy||Gynuity Health Projects||April 2013||Not Applicable|
|NCT00936741||Completed||Drug: mifepristone||Cushing''s Syndrome||Corcept Therapeutics||July 2009||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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