ARD-266

• CAT Number: I022397
• CAS Number: 2666951-70-6
• Molecular Formula: C52H59ClN6O7
• Molecular Weight: 915.51
• Purity: ≥95%
• Synonyms: (2S,4R)-N-[(1S)-3-[4-[2-[4-[[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]carbamoyl]phenyl]ethynyl]piperidin-1-yl]-3-oxo-1-phenylpropyl]-4-hydroxy-1-[(2R)-3-methyl-2-(3-methyl-1,2-oxazol-5-yl)butanoyl]pyrrolidine-2-carboxamide
• InChI: 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
• InChIKey: RTNONCBKGZNCJS-WPVVNVAYSA-N
• SMILES: CC1=NOC(=C1)C(C(C)C)C(=O)N2CC(CC2C(=O)NC(CC(=O)N3CCC(CC3)C#CC4=CC=C(C=C4)C(=O)NC5C(C(C5(C)C)OC6=CC(=C(C=C6)C#N)Cl)(C)C)C7=CC=CC=C7)O

ARD-266(CAT: I022397) is a highly potent androgen receptor (AR) PROTAC degrader that recruits the von Hippel–Lindau (VHL) E3 ligase for targeted protein degradation. It efficiently eliminates AR protein in AR-positive prostate cancer cell lines (LNCaP, VCaP, 22Rv1) with DC₅₀ values of 0.2–1 nM. In LNCaP cells, ARD-266 (100 nM) reduces AR within 3 h and achieves near-complete degradation by 6 h. It also downregulates AR-regulated genes (PSA, TMPRSS2, FKBP5) by >50% at 10 nM. ARD-266 contains an alkyne group, enabling click chemistry (CuAAC) conjugations, making it a versatile tool for chemical biology and AR-targeted cancer research.