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Description

A cell-permeable, bioavailable, non-toxic dihydroindolone derived compound that directly interacts with ERalpha and noncompetitively inhibits E2-ERalpha regulated gene expression. Selectively arrests the proliferation of therapy resistant ERalpha+ cancer cells (0.1 - 1.0 µ,M, IC50 = 15 nM for T47D cells) with no effect on ERalpha- cells. Shown to hyperactivate PLCgamma, deplete endoplasmic reticulum calcium store, elicit massive UPR, and inhibit protein synthesis continually. Downregulates chaperones synthesis and sustains UPR activated cell death. Rapidly induces tumor regression (>60% inhibition) in mouse MCF-7 xenografts (15 mg/kg, i.p., q.d.)., A cell-permeable, bioavailable, non-toxic dihydroindolone derived compound that directly interacts with ERalpha and noncompetitively inhibits E2-ERalpha regulated gene expression. Selectively arrests the proliferation of therapy resistant ERalpha+ cancer cells (0.1 - 1.0 µ,M, IC50 = 15 nM for T47D cells) with no effect on ERalpha- cells. Shown to hyperactivate PLCgamma, deplete endoplasmic reticulum calcium store, elicit massive UPR, and inhibit protein synthesis continually. Downregulates chaperones synthesis and sustains UPR activated cell death. Rapidly induces tumor regression (>60% inhibition) in mouse MCF-7 xenografts (15 mg/kg, i.p., q.d.).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.