(Rac)-Vepdegestrant

SKU: orb3143484

Description

(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.

Research Area

Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2229711-08-2
• MW: 723.90
• Formula: C₄₅H₄₉N₅O₄
• SMILES: 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
• Target: Estrogen Receptor/ERR,PROTACs

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR,PROTACs