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Estrogen receptor antagonist 2 is a degrader of estrogen receptor α (ERα).1 It induces degradation of ERα in MCF-7 breast cancer cells (IC50 = 0.16 nM). Estrogen receptor antagonist 2 inhibits estradiol-induced growth in MCF-7 cells (IC50 = 5.01 nM). In vivo, estrogen receptor antagonist 2 (0.5-50 mg/kg per day) decreases tumor volume in an MCF-7 mouse xenograft model.
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1. Discovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist. J. Med. Chem. 63(23), 14530-14559 (2020).