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ARCC-4

Chemical Structure : ARCC-4

CAS No.: 1973403-00-7

ARCC-4 (ARCC4)

Catalog No.: PC-22554Not For Human Use, Lab Use Only.

ARCC-4 is a potent, selective enzalutamide-based von Hippel-Lindau (VHL)-recruiting androgen receptor (AR) degrader with DC50 of 5 nM in VCaP cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ARCC-4 is a potent, selective enzalutamide-based von Hippel-Lindau (VHL)-recruiting androgen receptor (AR) degrader with DC50 of 5 nM in VCaP cells.
ARCC-4 is better at overcoming resistance in cellular models of castration-resistant prostate cancer (CRPC).
ARCC-4 is better than enzalutamide at inducing apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells.
ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy, and maintains its potency to degrade AR and inhibit cell proliferation in a high androgen environment in which enzalutamide has no activity.

Physicochemical Properties

M.Wt 1024.18
Formula C53H56F3N7O7S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Salami J, et al. Commun Biol. 2018 Aug 2;1:100.

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