PROTACERα Degrader-12 is a potent and highly selective ERα PROTAC degrader. It exhibits antiproliferative effects on various wild-type and mutant ERα breast cancer cell lines, causing cell cycle arrest and inducing apoptosis. PROTACERα Degrader-12 demonstrates excellent antitumor and ERα degradation activity and is suitable for breast cancer research.

PROTAC ERα Degrader-12 (Compound CP03) demonstrates significant degradation activity in MCF-7 cells at concentrations between 0.1-10 μM over 24 hours, with a DC50 value of 1.02 μM. Additionally, it exhibits notable antitumor activity in the same cell line at concentrations ranging from 0.01-100 μM with an IC50 of 0.17 μM. The compound shows exceptional stability in human liver microsomes and plasma with a plasma protein binding rate of 97.8%. When used at 1-5 μM for 48 hours in MCF-7 cells, PROTAC ERα Degrader-12 can arrest the cell cycle at the G1 phase and induces significant cell death and damage.

PROTAC ERα Degrader-12 (Compound CP03), administered intraperitoneally at doses of 1-4 mg/kg every other day for either 26 or 33 days, exhibits significant antitumor activity in mouse xenograft models of MCF-7 and LCC-2 tumors.