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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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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