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XY018

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Catalog No. T24213Cas No. 1873358-87-2
Alias XY-018, XY 018

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.

XY018

XY018

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Purity: 99.96%
Catalog No. T24213Alias XY-018, XY 018Cas No. 1873358-87-2
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
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
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.96%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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]
SynonymsXY-018, XY 018
Chemical Properties
Molecular Weight516.37
FormulaC23H15F7N2O4
Cas No.1873358-87-2
SmilesO=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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.9366 mL9.6830 mL19.3660 mL96.8298 mL
5 mM0.3873 mL1.9366 mL3.8732 mL19.3660 mL
10 mM0.1937 mL0.9683 mL1.9366 mL9.6830 mL
20 mM0.0968 mL0.4841 mL0.9683 mL4.8415 mL
50 mM0.0387 mL0.1937 mL0.3873 mL1.9366 mL
100 mM0.0194 mL0.0968 mL0.1937 mL0.9683 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
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Keywords

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