ERα degrader10 is a potent, selective, orally active estrogen receptor α (ERα) degrader. It demonstrates strong ERα binding affinity (IC50 of 24.0 nM) and degradation capability (EC50 of 5.3 nM). This compound degrades ERα through a proteasome-mediated pathway and is utilized in breast cancer research.

ERα:24 nM

ERα degrader 10 (compound A20) exhibits potent antiproliferative effects on MCF-7 cells with an IC 50 of 0.28 nM. Demonstrating concentration-dependent degradation of ERα, the optimum degradation occurs at 24 hours using a proteasome-mediated protein degradation pathway. Moreover, ERα degrader 10 (10-100 nM; 24 h) inhibits ERα signaling and induces cell cycle arrest at the G1 phase in MCF-7 cells.

ERα degrader 10 (10-30 mg/kg; oral gavage; once daily; for 30 days) demonstrated outstanding antitumor efficacy in the in vivo MCF-7 xenograft model.