(Rac)-ErSO-DFP

(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1)[1].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

IC50: 35 nM (MCF-7 cells)[1].

(Rac)-ErSO-DFP (compound 2) (0.001-1 µM; 24 h) maintains potent anticancer activity with IC50 of 35 nM in MCF-7 cells[1]. Cell Viability Assay[1] Cell Line: MCF-7 cells Concentration: 0.001-1 µM Incubation Time: 24 h Result: Showed a sustained activity of anticancer with IC50 of 35 nM.

(Rac)-ErSO-DFP (compound 2) (5 mg/kg; i.v.; 3xq.wk.) shows a sustained activity of againsting ERα+ breast cancer at low doses[1]. Animal Model: Ovariectomized Nu/J mice (MCF-7 orthotopic tumor model)[1]. Dosage: 5 mg/kg Administration: Intravenous injection; once-a-week for 3 total doses. Result: Maintained the ability to regress MCF-7 tumors in a mouse model of ERα+ breast cancer.

[1]. Hergenrother, et al. Enzyme-activating compounds and compositions. Patent WO2022087234A1.