ARCC 4

Name: ARCC 4
Brand: tocris
SKU: 7254

Catalog # 7254

Datasheet / COA / SDS

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Key Product Details

Description:	Potent and selective androgen receptor 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)
Molecular Weight:	1024.18

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Biological Activity

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 (D_max = 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) also available.

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

Technical Data

M. Wt	1024.18
Formula	C₅₃H₅₆F₃N₇O₇S₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1973403-00-7
InChi Key	DUPAJELXESPTNF-PPZGWQTASA-N
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

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

Preparing Stock Solutions

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	0.98 mL	4.88 mL	9.76 mL
5 mM	0.20 mL	0.98 mL	1.95 mL
10 mM	0.10 mL	0.49 mL	0.98 mL
50 mM	0.02 mL	0.10 mL	0.20 mL

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References

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

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