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Description: Potent and selective androgen receptor Degrader (PROTAC®)
Chemical Name: (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
Purity: ≥98% (HPLC)
Literature (2)

Biological Activity for ARCC 4

ARCC 4 is a potent and selective androgen receptor (AR) PROTAC® Degrader (DC50 = 5 nM). Comprises an androgen receptor antagonist, enzalutamide, joined by a linker to a VHL E3 ligase ligand. Brings about degradation of ARs in VCaP and LNCaP prostate cancer cell lines (Dmax = 98% at 12h) in a proteasome-dependent manner, and inhibits cell proliferation. Also degrades clinically relevant AR mutants expressed in HEK293T cells. Exhibits no significant effect on glucocorticoid, estrogen or progesterone receptors at concentrations inducing AR degradation.

ARCC 4 negative control (Cat. No. 7255) and R/NR3C4 antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # MAB58762.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for ARCC 4

M. Wt 1024.18
Formula C53H56F3N7O7S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1973403-00-7
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCCCOC4=CC=C(C5=CC=C(N6C(N(C7=CC(C(F)(F)F)=C(C#N)C=C7)C(C6(C)C)=O)=S)C=C5)C=C4)=O)=O)O)=O)SC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for ARCC 4

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 102.42 100

Preparing Stock Solutions for ARCC 4

The following data is based on the product molecular weight 1024.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for ARCC 4

References are publications that support the biological activity of the product.

Salami et al (2018) Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance. Commun.Biol. 1 100 PMID: 30271980

If you know of a relevant reference for ARCC 4, please let us know.

Keywords: ARCC 4, ARCC 4 supplier, ARCC4, PROTAC, PROTACs, active, degraders, degrades, androgen, receptors, AR, proteolysis-targeting, chimera, prostate, cancer, potent, selective, Androgen, Receptor, Degraders, 7254, Tocris Bioscience

Citations for ARCC 4

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Currently there are no citations for ARCC 4. Do you know of a great paper that uses ARCC 4 from Tocris? Please let us know.

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia