arv-471

Vepdegestrant (ARV-471) is a selective and highly potent estrogen receptor (ER, ESR1) PROTAC degrader with strong degrading activity against the ER protein. By directly degrading the ER protein rather than merely antagonizing its activity, vepdegestrant effectively inhibits the ER signaling pathway and demonstrates significant antitumor activity in ER-positive (ER⁺) breast cancer, with a DC50 value of approximately 2 nM. It is particularly effective against tumors harboring ESR1 mutations.

(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.

Vepdegestrant-d5 (ARV-471-d5) is the deuterium-labeled version of Vepdegestrant. Vepdegestrant (ARV-471) serves as an orally active estrogen receptor PROTAC degrader used in combating breast cancer. This heterobifunctional molecule facilitates the interaction between estrogen receptor α and the intracellular E3 ligase complex, leading to ubiquitination and subsequent degradation of the estrogen receptor via the proteasome. Vepdegestrant effectively degrades estrogen receptors in ER-positive breast cancer cell lines, with a DC50 of approximately 2 nM.