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ARD-266 is a proteolysis-targeting chimera (PROTAC) containing an androgen receptor antagonist conjugated to a VHL ligand via a piperidine-alkyne linker.1 It induces degradation of the androgen receptor in LNCaP, VCaP, and 22Rv1 prostate cancer cells with half-maximal degradation concentration (DC50) values of 0.54, 0.97, and 0.15 nM, respectively. ARD-266 inhibits the growth of LNCaP and VCaP cells (IC50s = 2 and 6 nM, respectively).
WARNING This product is not for human or veterinary use.
1. Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands. J. Med. Chem. 62(24), 11218-11231 (2019).