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ARCC-4 - CAS 1973403-00-7

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ARCC-4 is a PROTAC, acting as an androgen receptor degrader. ARCC-4 is a low-nanomolar androgen receptor degrader able to degrade about 95% of cellular androgen receptors. It inhibits prostate tumor cell proliferation, degrades clinically relevant androgen receptor point mutants and unlike enzalutamide, retains antiproliferative effect in a high androgen environment.

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Molecular Formula

C53H56F3N7O7S2

Molecular Weight

1024.18

ARCC-4

- Specification
  - Purity
    
    99%
    
    Solubility
    
    In DMSO: 200 mg/mL (195.28 mM; Need ultrasonic)
    
    Storage
    
    Powder, -20°C, 3 years; 4°C, 2 years; In solvent, -80°C, 6 months; -20°C, 1 month
    
    Shipping
    
    Room temperature in continental US; may vary elsewhere.
    
    IUPAC Name
    
    (2S,4R)-1-[(2S)-2-[[2-[4-[4-[4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]phenyl]phenoxy]butoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
    
    Synonyms
    
    ARCC-4; 1973403-00-7; (2S,4R)-1-((S)-2-(2-(4-((4'-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-[1,1'-biphenyl]-4-yl)oxy)butoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide; CHEMBL4540528; SCHEMBL17946930; DUPAJELXESPTNF-PPZGWQTASA-N; AKOS040741162; MS-31874; HY-130492; CS-0108331; EN300-7526556; Z3482428589; O1-(ABM-14 ether), O4-(Methylcarboxamide with AHPC) Butanediol; (2S,4R)-1-[(2S)-2-(2-{4-[(4'-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl}-[1,1'-biphenyl]-4-yl)oxy]butoxy}acetamido)-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide
- Properties
  - InChI Key
    
    NBHWEDHRTGEGEB-VKZLHUHRSA-N
    
    InChI
    
    InChI=1S/C53H56F3N7O7S2.H2O/c1-32-45(72-31-59-32)36-11-9-33(10-12-36)28-58-47(66)43-26-40(64)29-61(43)48(67)46(51(2,3)4)60-44(65)30-69-23-7-8-24-70-41-21-16-35(17-22-41)34-13-18-38(19-14-34)63-50(71)62(49(68)52(63,5)6)39-20-15-37(27-57)42(25-39)53(54,55)56;/h9-22,25,31,40,43,46,64H,7-8,23-24,26,28-30H2,1-6H3,(H,58,66)(H,60,65);1H2/t40-,43+,46-;/m1./s1
    
    Canonical SMILES
    
    CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)COCCCCOC4=CC=C(C=C4)C5=CC=C(C=C5)N6C(=S)N(C(=O)C6(C)C)C7=CC(=C(C=C7)C#N)C(F)(F)F)O.O
- Reference Reading
  - 1. Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance
    
    Taavi K Neklesa, Nick J Vitale, Jemilat Salami, Jing Wang, Ryan R Willard, Meizhong Jin, Donald P McDonnell, Craig M Crews, Shanique Alabi, Andrew P Crew, Hanqing Dong Commun Biol . 2018 Aug 2;1:100. doi: 10.1038/s42003-018-0105-8.
    
    The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional activity using competitive antagonists, such as enzalutamide remains a frontline therapy for prostate cancer management. However, the majority of patients eventually develop drug resistance. We propose that targeting the androgen receptor for degradation via Proteolysis Targeting Chimeras (PROTACs) will be a better therapeutic strategy for targeting androgen receptor signaling in prostate cancer cells. Here we perform a head-to-head comparison between a currently approved androgen receptor antagonist enzalutamide, and its PROTAC derivative, ARCC-4, across different cellular models of prostate cancer drug resistance. ARCC-4 is a low-nanomolar androgen receptor degrader able to degrade about 95% of cellular androgen receptors. ARCC-4 inhibits prostate tumor cell proliferation, degrades clinically relevant androgen receptor point mutants and unlike enzalutamide, retains antiproliferative effect in a high androgen environment. Thus, ARCC-4 exemplifies how protein degradation can address the drug resistance hurdles of enzalutamide.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 0.98 mL 4.88 mL 9.76 mL
    
    5 mM 0.2 mL 0.98 mL 1.95 mL
    
    10 mM 0.1 mL 0.49 mL 0.98 mL
    
    50 mM 0.02 mL 0.1 mL 0.2 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	0.98 mL	4.88 mL	9.76 mL
5 mM	0.2 mL	0.98 mL	1.95 mL
10 mM	0.1 mL	0.49 mL	0.98 mL
50 mM	0.02 mL	0.1 mL	0.2 mL

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