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).

Product information

CAS Number: 1873358-87-2

Molecular Weight: 516.37

Formula: C23H15F7N2O4

Chemical Name: N-[2'-fluoro-4'-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-[1,1'-biphenyl]-4-yl]-2-(2-nitrophenyl)acetamide

Smiles: [O-][N+](=O)C1=CC=CC=C1CC(=O)NC1C=CC(=CC=1)C1=CC=C(C=C1F)C(O)(C(F)(F)F)C(F)(F)F

InChiKey: MNVXADPCMINSEC-UHFFFAOYSA-N

InChi: InChI=1S/C23H15F7N2O4/c24-18-12-15(21(34,22(25,26)27)23(28,29)30)7-10-17(18)13-5-8-16(9-6-13)31-20(33)11-14-3-1-2-4-19(14)32(35)36/h1-10,12,34H,11H2,(H,31,33)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

XY018 (0.07-10 μM; 4 days) inhibit CRPC tumors C4-2B cells growth and survival. 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. 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.

In Vivo:

XY018 (5 mg/kg; intraperitoneally i.p.; five times per week for 23 days) inhibit CRPC tumor growth in mice . XY018 (10 mg/kg orally or 2 mg/kg intravenously) exhibits reasonable pharmacokinetics profiles in SD rats.

Products are for research use only. Not for human use.