For research use only. Not for therapeutic Use.
ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor[1].
ARD-2585 achieves DC50 values of 0.04-0.1 nM in the VCaP cell line with AR gene amplification and in the LNCaP cell line carrying an AR mutation[1].
ARD-2585 (100 nM) is effective in reducing the AR protein level at the 3 and 24 h time-points by 78% (p < 0.01) and 60% at the 6 h time-point (p > 0.05)[1].
| Catalog Number | I044404 |
| CAS Number | 2757422-79-8 |
| Synonyms | N-[4-(3-chloro-4-cyano-N-methylanilino)cyclohexyl]-4-[4-[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]azetidin-3-yl]piperazin-1-yl]benzamide |
| Molecular Formula | C41H43ClN8O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C41H43ClN8O5/c1-46(30-9-4-26(22-43)35(42)21-30)28-10-5-27(6-11-28)44-38(52)25-2-7-29(8-3-25)47-16-18-48(19-17-47)32-23-49(24-32)31-12-13-33-34(20-31)41(55)50(40(33)54)36-14-15-37(51)45-39(36)53/h2-4,7-9,12-13,20-21,27-28,32,36H,5-6,10-11,14-19,23-24H2,1H3,(H,44,52)(H,45,51,53) |
| InChIKey | LUCHABJUYSYJAT-UHFFFAOYSA-N |
| SMILES | CN(C1CCC(CC1)NC(=O)C2=CC=C(C=C2)N3CCN(CC3)C4CN(C4)C5=CC6=C(C=C5)C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC(=C(C=C8)C#N)Cl |
| Reference | [1]. Weiguo Xiang. et al. Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2021 Sep 23;64(18):13487-13509. |
