ARCC 4
Tocris Bioscience, part of Bio-Techne | Catalog # 7254
Potent and selective androgen receptor Degrader (PROTAC®)
Key Product Details
Description
Potent and selective androgen receptor Degrader (PROTAC®)
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background 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
Product Specific Notices for ARCC 4
For research use only
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