BY13

BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR) ) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant. BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model[1]. Pink: SRC-3 ligand (SI-2) (HY-101447) ; Blue: CRBN ligase ligand (HY-41547) ; Black: linker (HY-176226)

C35H35N9O4

645.71

C/C(C1=NC=CC=C1)=N\NC2=NC(C=CC=C3)=C3N2C4CN(C4)C5CCN(CC5)C6=CC=CC7=C6C(N(C7=O)C8C(NC(CC8)=O)=O)=O

Apoptosis; Estrogen Receptor/ERR; PROTACs; Src

ERα; SRC-3

Room temperature