PROTAC ERα Degrader-9

SKU: orb3134700

Description

PROTACERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader designed to diminish estrogen receptor α (ERα) and aromatase (ARO). It demonstrates a Ki of 0.25 μM for ERα binding and an IC50 of 4.6 μM for ARO inhibition. This compound curbs proliferation in wild-type MCF-7 cells (IC50=0.54 μM) and ERα mutant variants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), and MCF-7Y537S (IC50=2.3 μM), while also downregulating ERS1 and MYC expression. PROTACERα Degrader-9 arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7 cells, exhibiting antitumor efficacy in mouse models.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• Formula: C₅₈H₆₄F₃N₇O₉S₂
• Target: Cytochromes P450,Estrogen Receptor/ERR,PROTACs,Apoptosis

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Cytochromes P450,Estrogen Receptor/ERR,PROTACs,Apoptosis