Mifepristone

Mifepristone is an antagonist of glucocorticoid, progesterone, and androgen receptors (Kis = 0.1, 0.64, and 0.65 nM, respectively). It is selective for these receptors over the mineralocorticoid receptor (MR), estrogen receptor alpha (ERalpha), and ERbeta (Kis = 640, >200, and >750 nM, respectively). In cell-based assays, mifepristone inhibits alkaline phosphatase activity stimulated by the progesterone receptor agonist R5020 as well as reporter transcription stimulated by either dexamethasone (Cay-11015) or R5020 (IC50s = 7, 5.9, and 1.3 nM, respectively). It also inhibits synthetic androgen R1881-stimulated reporter transcription in a concentration-dependent manner. Mifepristone (10 µM) inhibits growth of 4-OHT-resistant MCF-7 breast cancer cells in vitro. It also inhibits tumor growth in an SKOV3 ovarian cancer nude mouse xenograft model when administered at doses of 0.5 or 1 mg per day. Formulations containing mifepristone have been used for the induction of medical abortions.Formal Name: 11beta-[4-(dimethylamino)phenyl]-17beta-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one. CAS Number: 84371-65-3. Synonyms: RU-486. Molecular Formula: C29H35NO2. Formula Weight: 429.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2)(1:4): .2 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml, Methanol: 1 mg/ml. lambdamax: 261, 303 nm. SMILES: CN(C)C1=CC=C(C=C1)[C@H]2C[C@@]3(C)[C@](CC[C@]3(C#CC)O)([H])[C@]4([H])CCC5=CC(CCC5=C42)=O. InChi Code: InChI=1S/C29H35NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26,29)2)19-6-9-21(10-7-19)30(3)4/h6-7,9-10,17,24-26,32H,8,11-14,16,18H2,1-4H3/t24-,25+,26-,28-,29-/m0/s1. InChi Key: VKHAHZOOUSRJNA-GCNJZUOMSA-N.