(Rac) -Vepdegestrant

(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.