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XY018 

Cat. No.: HY-120210 Purity: 99.76%
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).

For research use only. We do not sell to patients.

XY018 Chemical Structure

XY018 Chemical Structure

CAS No. : 1873358-87-2

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10 mM * 1 mL in DMSO USD 125 In-stock
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100 mg USD 950 In-stock
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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9366 mL 9.6830 mL 19.3660 mL
5 mM 0.3873 mL 1.9366 mL 3.8732 mL
10 mM 0.1937 mL 0.9683 mL 1.9366 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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