| Identification | Back Directory | [Name]
N-[2'-Fluoro-4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'biphenyl]-4-yl]-2-nitrobenzeneacetamide | [CAS]
1873358-87-2 | [Synonyms]
N-[2'-Fluoro-4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'biphenyl]-4-yl]-2-nitrobenzeneacetamide
Benzeneacetamide, N-[2'-fluoro-4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'-biphenyl]-4-yl]-2-nitro- | [Molecular Formula]
C23H15F7N2O4 | [MOL File]
1873358-87-2.mol | [Molecular Weight]
516.36 |
| Chemical Properties | Back Directory | [Boiling point ]
613.0±55.0 °C(Predicted) | [density ]
1.496±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
8.87±0.19(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
XY 018 is a RORγ antagonist (EC50 = 190 nM). XY 018 suppresses androgen receptor expression in prostate cancer cell lines. Also inhibits growth of tumors in androgen receptor-positive xenograft models. | [in vivo]
XY018 (5 mg/kg; intraperitoneally i.p.; five times per week for 23 days) inhibit CRPC tumor growth in mice[1] .
XY018 (10 mg/kg orally or 2 mg/kg intravenously) exhibits reasonable pharmacokinetics profiles in SD rats[2]. | Animal Model: | Four-week-old male SCID C.B17 mice (for C4-2B and VCaP) or BALB/c nu/nu athymic mice (for 22Rv1 and PC-3)[1] | | Dosage: | 5 mg/kg | | Administration: | Treated intraperitoneally (i.p.); five times per week for 23 days | | Result: | Tumor growth inhibition. |
| Animal Model: | Sprague Dawley rats[2] | | Dosage: | 10 mg/kg (po; 1 mg/mL); 2 mg/kg (iv;0.4 mg/mL) (Pharmacokinetic Analysis) | | Administration: | Orally administrated (10 mg/kg) and intravenously administrated (2 mg/kg); single dose | | Result: | High plasma exposure AUC(0–∞) value of 6444 (μg/L·h), half-life (T1/2=7.67±2.36 h) and maximum plasma concentration (Cmax) value of 839 (μg/L) after a 2 mg/kg iv administration.
Demonstrated a relatively low oral bioavailability of 19% after an oral administration. |
| [IC 50]
ROR-γ: 0.19 μM (IC50, in 293 T cells); ROR-α: 7.57 μM (IC50, in 293 T cells) | [storage]
Store at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|