Fulvestrant

Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor alpha (ERalpha). It binds to rat uterine ER with an IC50 value of 44.8 nM and prevents uterine weight increases induced by estradiol in immature rats (ED50> = 0.06 mg/kg per day) but has no effect on uterine weight alone. It also decreases uterine weight in adult rats without affecting the production of luteinizing and follicle-stimulating hormones and prolactin. Fulvestrant inhibits the growth of ER-positive MCF-7 human breast cancer cells but not ER-negative BT-20 cells when used at a concentration of 1 µg/ml. It also prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models when used at a single dose of 5 mg per animal. Fulvestrant is neuroprotective in vitro against neurotoxicity induced by glutamate- and amyloid-beta (1-42) (Abeta42) in primary rat hippocampal cells. Formulations containing fulvestrant have been used in the treatment of estrogen-sensitive breast cancer.Formal Name: 7alpha-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3,17beta-diol. CAS Number: 129453-61-8. Synonyms: ICI 182780. Molecular Formula: C32H47F5O3S. Formula Weight: 606.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, Ethanol: 25 mg/ml. lambdamax: 282 nm. SMILES: OC1=CC=C2C(C[C@@H](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)[C@]3([H])[C@]2([H])CC[C@@]4(C)C3CC[C@@H]4O)=C1. InChi Code: InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27?,28+,29-,30+,41?/m1/s1. InChi Key: VWUXBMIQPBEWFH-HNWKPAMESA-N.