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PROTAC ERα Degrader-9

CAT: 0931-T210250-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T210250-01Size:10 mg
Selected
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Quick Request Actions
Target
PROTACs, Apoptosis, Cytochromes P450, Estrogen Receptor/ERR
Related Pathways
Apoptosis, PROTAC, Endocrinology/Hormones, Metabolism
Bioactivity
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.
Molecular Formula
C58H64F3N7O9S2
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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