For research use only. Not for therapeutic Use.
ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer[1].
Catalog Number | I040940 |
CAS Number | 2632305-17-8 |
Synonyms | 2-chloro-4-[(3S)-8-[4-[4-[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]azetidin-3-yl]piperazine-1-carbonyl]phenyl]-3-methyl-2,8-diazaspiro[4.5]decan-2-yl]benzonitrile |
Molecular Formula | C43H45ClN8O5 |
Purity | ≥95% |
InChI | InChI=1S/C43H45ClN8O5/c1-27-22-43(26-51(27)32-7-4-29(23-45)36(44)21-32)12-14-47(15-13-43)30-5-2-28(3-6-30)40(55)49-18-16-48(17-19-49)33-24-50(25-33)31-8-9-34-35(20-31)42(57)52(41(34)56)37-10-11-38(53)46-39(37)54/h2-9,20-21,27,33,37H,10-19,22,24-26H2,1H3,(H,46,53,54)/t27-,37?/m0/s1 |
InChIKey | WBMJNGGUHCHFHY-YTCZSSRZSA-N |
SMILES | CC1CC2(CCN(CC2)C3=CC=C(C=C3)C(=O)N4CCN(CC4)C5CN(C5)C6=CC7=C(C=C6)C(=O)N(C7=O)C8CCC(=O)NC8=O)CN1C9=CC(=C(C=C9)C#N)Cl |
Reference | [1]. Han X, et al. Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2023 Jul 13;66(13):8822-8843. |