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Key Product Details
| Description: | Potent and selective androgen receptor degrader |
| 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 |
Biological Activity
Potent and selective androgen receptor (AR) 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) also available.
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 | |||
| 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
Citations
Currently there are no citations for ARCC 4.
