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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.
Pack Size | Price | Availability | Quantity |
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10 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | 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. |
Targets&IC50 | ERα:24 nM |
In vitro | 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. |
In vivo | 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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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