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G1T48 is a potent selective estrogen receptor downregulator (SERD). a Chemical structures of G1T48 and benchmark SERMs and SERDs. b G1T48 downregulates the estrogen receptor in breast cancer cells. MCF7 cells were treated with ER ligands (10–12–10–6 M) for 18 h prior to fixation and detection of ER levels by In-Cell Western. *For tamoxifen and GW5638, dose response was 10–11–10–5 M. Error bars indicate the SD of triplicate samples
