era degrader-2

ERα degrader-2 是一种具有选择性和有效性的雌激素受体 (SERD)降解剂，具有抗癌活性，抑制 ERα，对雌激素受体降解的 EC50 值为 0.3 nM。ERα degrader-2 可用于预防和治疗 HER 阳性乳腺癌。

PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].