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Submit ReviewXY 018
Description: RORγ antagonist; inhibits AR expression
Chemical Name: N-[2'-Fluoro-4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'biphenyl]-4-yl]-2-nitrobenzeneacetamide
Purity: ≥98% (HPLC)
Biological Activity
RORγ antagonist (EC50 = 190 nM). Suppresses androgen receptor expression in prostate cancer cell lines. Also inhibits growth of tumors in androgen receptor-positive xenograft models.
Technical Data
| M. Wt | 516.36 |
| Formula | C23H15F7N2O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1873358-87-2 |
| PubChem ID | 130248006 |
| InChI Key | MNVXADPCMINSEC-UHFFFAOYSA-N |
| Smiles | OC(C(F)(F)F)(C(F)(F)F)C1=CC(F)=C(C2=CC=C(C=C2)NC(CC3=C([N+]([O-])=O)C=CC=C3)=O)C=C1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.64 | 100 | |
| ethanol | 51.64 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 516.36. 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 | 1.94 mL | 9.68 mL | 19.37 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.87 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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References
References are publications that support the biological activity of the product.
Wang et al (2016) ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer. Nat.Med. 22 488 PMID: 27019329
Ndagi et al (2016) Re-emergence of an orphan therapeutic target for the treatment of resistant prostate cancer - a through conformational and binding analysis for RORγ protein. J.Biomol.Struct.Dyn. 36 1
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Nuclear Receptors Product Listing
A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:
- Androgen Receptors
- Estrogen Receptors
- Retinoic Acid Receptors
- Retinoid X Receptors
- Vitamin D Receptors