For research use only. Not for therapeutic Use.
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models[1].
The DC50 values of ARD-1676 for AR degradation in AR+ VCaP and LNCaP cell lines are 0.1 and 1.1 nM, respectively, and the IC50 values in VCaP and LNCaP cell lines are 11.5 and 2.8 nM respectively[1].
The oral bioavailability of ARD-1676 was 67%, 44%, 31%, and 99% in mice, rats, dogs, and monkeys, respectively. ARD-1676 effectively reduces AR protein levels in mouse VCaP tumor tissues and inhibits tumor growth in VCaP mouse xenograft tumor models[1].
| Catalog Number | I040684 |
| CAS Number | 2632305-36-1 |
| Synonyms | 2-chloro-4-[(3S)-8-[4-[4-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-5,7-dihydropyrrolo[3,4-f]isoindol-6-yl]methyl]piperidine-1-carbonyl]phenyl]-3-methyl-2,8-diazaspiro[4.5]decan-2-yl]benzonitrile |
| Molecular Formula | C44H46ClN7O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C44H46ClN7O5/c1-27-21-44(26-51(27)34-7-4-30(22-46)37(45)20-34)12-16-49(17-13-44)33-5-2-29(3-6-33)41(55)50-14-10-28(11-15-50)23-48-24-31-18-35-36(19-32(31)25-48)43(57)52(42(35)56)38-8-9-39(53)47-40(38)54/h2-7,18-20,27-28,38H,8-17,21,23-26H2,1H3,(H,47,53,54)/t27-,38?/m0/s1 |
| InChIKey | GAXWAKXJBZHVQF-ZVENJKCTSA-N |
| SMILES | CC1CC2(CCN(CC2)C3=CC=C(C=C3)C(=O)N4CCC(CC4)CN5CC6=CC7=C(C=C6C5)C(=O)N(C7=O)C8CCC(=O)NC8=O)CN1C9=CC(=C(C=C9)C#N)Cl |
| Reference | [1]. Xiang W, et al. Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer. J Med Chem. 2023 Sep 8.. |
