ARD-266

ARD-266 is a proteolysis-targeting chimera (PROTAC) containing an androgen receptor antagonist conjugated to a VHL ligand via a piperidine-alkyne linker. 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). SMILES: CC(C)([C@H](C1(C)C)NC(C2=CC=C(C=C2)C#CC3CCN(CC3)C(C[C@@H](C4=CC=CC=C4)NC([C@H]5N(C[C@@H](C5)O)C([C@@H](C6=CC(C)=NO6)C(C)C)=O)=O)=O)=O)[C@H]1OC7=CC(Cl)=C(C=C7)C#N. InChi Code: InChI=1S/C52H59ClN6O7/c1-31(2)45(43-25-32(3)57-66-43)48(64)59-30-38(60)26-42(59)47(63)55-41(35-11-9-8-10-12-35)28-44(61)58-23-21-34(22-24-58)14-13-33-15-17-36(18-16-33)46(62)56-49-51(4,5)50(52(49,6)7)65-39-20-19-37(29-54)40(53)27-39/h8-12,15-20,25,27,31,34,38,41-42,45,49-50,60H,21-24,26,28,30H2,1-7H3,(H,55,63)(H,56,62)/t38-,41+,42+,45-,49-,50-/m1/s1. InChi Key: RTNONCBKGZNCJS-LJLQSONVSA-N