BY13

Description

BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 ?M. BY13 selectively blocks the ER signaling pathway over that of androgen receptor AR through down-regulating ER? level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant HY-13636 . BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model. Pink: SRC-3 ligand SI-2 HY-101447 ; Blue: CRBN ligase ligand HY-41547 ; Black: linker HY-176226