ARCC 4

Tocris Bioscience | Catalog # 7254

Potent and selective androgen receptor Degrader (PROTAC®)
Tocris Bioscience

Key Product Details

Description

Potent and selective androgen receptor Degrader (PROTAC®)
View all Active Degraders »

Product Description

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.

Product Specifications for ARCC 4

Molecular Weight

1024.18

Formula

C53H56F3N7O7S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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 all 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 0.20 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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 10 publications citing the usage of this product.

Product Documents for ARCC 4

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for ARCC 4

For research use only

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