(Rac) -Vepdegestrant

2229711-08-2

Estrogen Receptor/ERR, PROTACs

Endocrinology/Hormones, PROTAC

(Rac) -Vepdegestrant is an isomer of Vepdegestrant. Vepdegestrant ((Rac) -ARV-471) is an orally active estrogen receptor PROTAC degrader used against breast cancer. It is a heterobifunctional molecule that facilitates the interaction between estrogen receptor α and the intracellular E3 ligase complex. Vepdegestrant induces ubiquitination and subsequent degradation of the estrogen receptor via the proteasome, effectively degrading ER in ER-positive breast cancer cell lines with a DC50 value of approximately 2 nM.

OC=1C=C2C([C@H]([C@H](CC2)C3=CC=CC=C3)C4=CC=C(C=C4)N5CCC(CN6CCN(CC6)C=7C=C8C(=CC7)C(=O)N(C8)C9C(=O)NC(=O)CC9)CC5)=CC1

C45H49N5O4

723.9

Ice Packs

-20°C