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ARD-69 - CAS 2316837-10-0

Inquiry

It is a highly potent PROTAC degrader of androgen receptor (AR), which can reduce AR protein level in prostate cancer cell lines and effectively inhibit AR regulated gene expression. It effectively inhibits the growth of AR positive prostate cancer cells.

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Molecular Formula

C62H74ClFN8O7S

Molecular Weight

1129.82

ARD-69

- Specification
  - Purity
    
    ≥95%
    
    Solubility
    
    Soluble in DMSO
    
    Appearance
    
    Solid Powder
    
    Storage
    
    Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
    
    IUPAC Name
    
    (2S,4R)-N-((S)-3-(4-((4-(((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)carbamoyl)phenyl)ethynyl)-[1,4'-bipiperidin]-1'-yl)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
    
    Synonyms
    
    N-[(1-Fluorocyclopropyl)carbonyl]-3-methyl-L-valyl-(4R)-N-{(1S)-3-{4-[(4-{[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]carbamoyl}phenyl)ethynyl]-1,4'-bipiperidin-1'-yl}-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxopropyl}-4-hydroxy-L-prolinamide; L-Prolinamide, N-[(1-fluorocyclopropyl)carbonyl]-3-methyl-L-valyl-N-[(1S)-3-[4-[2-[4-[[[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]amino]carbonyl]phenyl]ethynyl][1,4'-bipiperidin]-1'-yl]-1-[4-(4-methyl-5-thiazolyl)phenyl]-3-oxopropyl]-4-hydroxy-, (4R)-; (2S,4R)-N-[(1S)-3-[4-[4-[2-[4-[[(1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]carbamoyl]phenyl]ethynyl]piperidin-1-yl]piperidin-1-yl]-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxopropyl]-1-[(2S)-2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide; ARD69; ARD 69
- Properties
  - Density
    
    1.34±0.1 g/cm3
    
    InChI Key
    
    CWGVEMFBQJUWLU-RXFAPWBBSA-N
    
    InChI
    
    InChI=1S/C62H74ClFN8O7S/c1-37-51(80-36-66-37)41-17-15-40(16-18-41)48(67-54(76)49-31-45(73)35-72(49)55(77)52(59(2,3)4)68-58(78)62(64)25-26-62)33-50(74)71-29-23-44(24-30-71)70-27-21-39(22-28-70)10-9-38-11-13-42(14-12-38)53(75)69-56-60(5,6)57(61(56,7)8)79-46-20-19-43(34-65)47(63)32-46/h11-20,32,36,39,44-45,48-49,52,56-57,73H,21-31,33,35H2,1-8H3,(H,67,76)(H,68,78)(H,69,75)/t45-,48+,49+,52-,56-,57-/m1/s1
    
    Canonical SMILES
    
    N#CC1=CC=C(OC2C(C)(C)C(NC(=O)C3=CC=C(C#CC4CCN(CC4)C5CCN(C(=O)CC(NC(=O)C6N(C(=O)C(NC(=O)C7(F)CC7)C(C)(C)C)CC(O)C6)C=8C=CC(=CC8)C=9SC=NC9C)CC5)C=C3)C2(C)C)C=C1Cl
- Reference Reading
  - 1. Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer.
    
    Han, X., Wang, C., Qin, C., Xiang, W., Fernandez-Salas, E., Yang, C.Y., Wang, M., Zhao, L., Xu, T., Chinnaswamy, K. and Delproposto, J., 2019. Journal of medicinal chemistry, 62(2), pp.941-964.
    
    We report herein the discovery of highly potent PROTAC degraders of androgen receptor (AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent manner. ARD-69 achieves DC50 values of 0.86, 0.76, and 10.4 nM in LNCaP, VCaP, and 22Rv1 AR+ prostate cancer cell lines, respectively. ARD-69 is capable of reducing the AR protein level by >95% in these prostate cancer cell lines and effectively suppressing AR-regulated gene expression. ARD-69 potently inhibits cell growth in these AR-positive prostate cancer cell lines and is >100 times more potent than AR antagonists. A single dose of ARD-69 effectively reduces the level of AR protein in xenograft tumor tissue in mice. Further optimization of ARD-69 may ultimately lead to a new therapy for AR+, castration-resistant prostate cancer.

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