Fulvestrant

White or off white crystalline powder. Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (20mg/ml). Chemical. CAS: 129453-61-8. Formula: C32H47F5O3S. MW: 606.77. Synthetic. Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor alpha (ERalpha). It reduces dimerization and nuclear localization of the estrogen receptor (ER). Fulvestrant lowers the level of ER protein in human breast cancer cells. 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 1µg/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.