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XY018 

Cat. No.: HY-120210
Handling Instructions

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).

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XY018 Chemical Structure

XY018 Chemical Structure

CAS No. : 1873358-87-2

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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].

IC50 & Target[1][2]

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.
Molecular Weight

516.37

Formula

C₂₃H₁₅F₇N₂O₄

CAS No.

1873358-87-2

SMILES

OC(C(F)(F)F)(C1=CC(F)=C(C(C=C2)=CC=C2NC(CC(C=CC=C3)=C3[N](=O)=O)=O)C=C1)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

XY018XY 018XY-018RORRAR-related orphan receptorROR-γ293TLBDcastration-resistantprostatecancerInhibitorinhibitorinhibit

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