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Elacestrant is a selective estrogen receptor degrader (SERD).1 It selectively binds to estrogen receptor α (ERα) over ERβ (IC50s = 48 and 870 nM, respectively) and reduces ERα levels in MCF-7 cells (EC50 = 0.6 nM). Elacestrant reduces MCF-7 proliferation induced by 17β-estradiol (E2; Item No. 10006315) (EC50 = 4 pM). In vivo, elacestrant (30 and 60 mg/kg) reduces E2-induced tumor growth in an MCF-7 mouse xenograft model. It increases survival in an MCF-7 intracranial mouse xenograft model. Elacestrant (0.1-3 mg/kg) protects against bone loss in ovariectomized rats.
WARNING This product is not for human or veterinary use.
1. RAD1901: A novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs 26(9), 948-956 (2015).