erα degrader 2

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

ER Degrader 2, a potent estrogen receptor (ER) degrader, plays a significant role in the estrogen signaling system, which is crucial for regulating cell growth, differentiation, and apoptosis. It holds promise for research in cancer diseases[1].

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].