|PROTAC ERα Degrader-2
|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).
|PROTAC ERα Degrader-1
|PROTAC ERα Degrader-1 is a PROTAC targeting ERα.
|ARV-471 is the first-clinical-entered ERα PROTAC degrader with DC50 of ~1nM. It degrades clinically-relevant ESR1 variants (Y537S and D538G) and inhibits growth of cell lines expressing those variants.