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XY018 is an orally available, selective and highly effective ROR-γ antagonist with antitumor activity, inhibits ROR-γ activity, inhibits tumor cell growth, and can be used to study drug-resistant prostate cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $38 | - | In Stock | |
| 5 mg | $82 | - | In Stock | |
| 10 mg | $118 | - | In Stock | |
| 25 mg | $193 | - | In Stock | |
| 50 mg | $286 | - | In Stock | |
| 100 mg | $423 | - | In Stock | |
| 200 mg | $629 | - | In Stock |
| Description | XY018 is an orally available, selective and highly effective ROR-γ antagonist with antitumor activity, inhibits ROR-γ activity, inhibits tumor cell growth, and can be used to study drug-resistant prostate cancer. |
| Targets&IC50 | RORα:7.57 μM (PME-1 (HEK293T)), RORγ:0.19 μM (PME-1 (HEK293T)) |
| In vitro | METHODS: C4-2B cells were treated with XY018 (0.07, 0.15, 0.31, 0.62, 1.25, 2.5, 5, 10 μM for 4 days), the cell titer GLO reagent was added, and cell viability was measured by luminescence on a GLOMAX microplate luminometer according to the manufacturer's instructions. RESULTS:XY018 inhibited the growth and survival of C4-2B cells. [1] |
| In vivo | METHODS: XY018 (5 mg/kg, intraperitoneal injection, 5 times a week for 23 days) was used to treat xenograft tumor model mice generated using PCa cell lines with different characteristics (such as C4-2B expressing AR with mutant LBD, VCaP and AR-V7 with amplified AR genes, 22Rv1 expressing high levels of multiple AR variants, and AR-negative PC3), and tumor growth in mice was observed. RESULTS:XY018 inhibited CRPC tumor growth in mice. [1] METHODS: XY018 (10 mg/kg, oral; 2 mg/kg, intravenous) was used to treat SD rats and its pharmacokinetic characteristics were determined. RESULTS:XY018 showed good pharmacokinetic characteristics in rats, with the same bioavailability of 19%, and an intravenous half-life of 7.67 hours. [2] |
| Synonyms | XY-018, XY 018 |
| Molecular Weight | 516.37 |
| Formula | C23H15F7N2O4 |
| Cas No. | 1873358-87-2 |
| Smiles | O=C(CC1=C([N+]([O-])=O)C=CC=C1)NC2=CC=C(C3=CC=C(C(C(F)(F)F)(C(F)(F)F)O)C=C3F)C=C2 |
| Relative Density. | 1.496 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (154.93 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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