ARD-2128

• CAT Number: I045391
• CAS Number: 2222111-87-5
• Molecular Formula: C45H50ClN7O6
• Molecular Weight: 820.37
• Purity: ≥95%
• Synonyms: N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperidin-4-yl]methyl]piperazin-1-yl]benzamide
• InChI: InChI=1S/C45H50ClN7O6/c1-44(2)42(45(3,4)43(44)59-32-11-7-29(25-47)35(46)24-32)49-38(55)28-5-8-30(9-6-28)52-21-19-50(20-22-52)26-27-15-17-51(18-16-27)31-10-12-33-34(23-31)41(58)53(40(33)57)36-13-14-37(54)48-39(36)56/h5-12,23-24,27,36,42-43H,13-22,26H2,1-4H3,(H,49,55)(H,48,54,56)
• InChIKey: BWDWHHAZFQBJQL-UHFFFAOYSA-N
• SMILES: CC1(C(C(C1OC2=CC(=C(C=C2)C#N)Cl)(C)C)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5CCN(CC5)C6=CC7=C(C=C6)C(=O)N(C7=O)C8CCC(=O)NC8=O)C

ARD-2128 (Cat No.: I045391) is an investigational proteolysis-targeting chimera (PROTAC) designed to selectively degrade androgen receptor (AR) protein, including mutant and splice variant forms like AR-V7, which are implicated in castration-resistant prostate cancer (CRPC). By harnessing the cell’s ubiquitin-proteasome system, ARD-2128 binds AR and recruits an E3 ligase to trigger targeted degradation, effectively shutting down AR-driven transcription. This mechanism overcomes limitations of conventional AR inhibitors. ARD-2128 is being studied in preclinical models as a promising therapy for advanced prostate cancers resistant to standard treatments.

Reference

[1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00882.
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