1873358-87-2
1873358-87-2 structure
- Name: XY 018
- Chemical Name: XY018
- CAS Number: 1873358-87-2
- Molecular Formula: C23H15F7N2O4
- Molecular Weight: 516.37
- Catalog: Signaling Pathways Metabolic Enzyme/Protease ROR
- Create Date: 2020-06-01 08:27:43
- Modify Date: 2024-01-14 20:52:53
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XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD)[1].
| Name | XY018 |
|---|
| Description | XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD)[1]. |
|---|---|
| Related Catalog | |
| Target |
ROR-γ:0.19 μM (IC50, in 293 T cells) ROR-α:7.57 μM (IC50, in 293 T cells) |
| In Vitro | XY018 (0.07-10 μM; 4 days) inhibit CRPC tumors C4-2B cells growth and survival[1]. XY018 inhibits Gal4-RORγ-LBD and Gal4-RORα-LBD with IC50s of 0.19±0.02 and 7.57 μM in 293 T cells, respectively[2]. XY018 shows anti-proliferation effects against the prostate cancer cell lines LNCaP, 22Rv1, C4-2B, DU145, and PC-3 with IC50s of 5.14±0.36, 9.00±0.33, 9.20, 28.43±0.89, and 11.14±1.78 μM, respectively[2]. Cell Viability Assay[1] Cell Line: CRPC tumors C4-2B Concentration: 0.07, 0.15, 0.31, 0.62, 1.25, 2.5, 5, and 10 μM Incubation Time: 4 days Result: Inhibited growth and survival. |
| 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. |
| References |
| Molecular Formula | C23H15F7N2O4 |
|---|---|
| Molecular Weight | 516.37 |