Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor alpha (ERalpha).1,2 It binds to rat uterine ER with an IC50 value of 44.8nM and prevents uterine weight increases induced by estradiol in immature rats (ED50> = 0.06mg/kg per day) but has no effect on uterine weight alone.3 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 1ug/ml. It also prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models when used at a single dose of 5mg per animal. Fulvestrant is neuroprotective in vitro against neurotoxicity induced by glutamate- and amyloid-beta (1-42) (Abeta42) in primary rat hippocampal cells.4 Formulations containing fulvestrant have been used in the treatment of estrogen-sensitive breast cancer. Synonyms (7alpha,17beta)-7-[9-[4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol, Faslodex, Fulvestrant, ICI 182780, ZD 182780, ZD 9238, ZM 182780 CAS Number: 129453-61-8 Molecular Formula: C32H47F5O3S Molecular Weight:: 606.77 Appearance: White to off-white crystalline powder Purity: 99% Specific optical rotation [alpha]20D.3 (c=2, CH OH): +108 to 115 Loss on Drying: 0.5% Melting Point: 101-108C Solubility: Dichloromethane (Slightly), DMSO (Slightly), Ethanol (Slightly), Methanol (Slightly) Storage: -20C
Molekulargewicht:
606.77
Reinheit:
99%
Formulierung:
White to off-white crystalline powder
CAS Nummer:
[129453-61-8]
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