2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. XY018

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 125 In-stock
Solution
10 mM * 1 mL in DMSO USD 125 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 180 In-stock
50 mg USD 600 In-stock
100 mg USD 950 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

XY018 Related Antibodies

Top Publications Citing Use of Products

View All ROR Isoform Specific Products:

View All Isoforms
RORγ RORα RORβ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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)

Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
9 μM
Compound: 23; XY018
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
DU-145 IC50
28.43 μM
Compound: 23; XY018
Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay
[PMID: 30964293]
LNCaP IC50
5.14 μM
Compound: 23; XY018
Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
LNCaP C4-2B IC50
9.2 μM
Compound: 23; XY018
Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
PC-3 IC50
11.14 μM
Compound: 23; XY018
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
[PMID: 30964293]
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].

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

XY018 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9366 mL 9.6830 mL 19.3660 mL 48.4149 mL
5 mM 0.3873 mL 1.9366 mL 3.8732 mL 9.6830 mL
10 mM 0.1937 mL 0.9683 mL 1.9366 mL 4.8415 mL
15 mM 0.1291 mL 0.6455 mL 1.2911 mL 3.2277 mL
20 mM 0.0968 mL 0.4841 mL 0.9683 mL 2.4207 mL
25 mM 0.0775 mL 0.3873 mL 0.7746 mL 1.9366 mL
30 mM 0.0646 mL 0.3228 mL 0.6455 mL 1.6138 mL
40 mM 0.0484 mL 0.2421 mL 0.4841 mL 1.2104 mL
50 mM 0.0387 mL 0.1937 mL 0.3873 mL 0.9683 mL
60 mM 0.0323 mL 0.1614 mL 0.3228 mL 0.8069 mL
80 mM 0.0242 mL 0.1210 mL 0.2421 mL 0.6052 mL
100 mM 0.0194 mL 0.0968 mL 0.1937 mL 0.4841 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

XY018 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XY0181873358-87-2XY 018XY-018RORRAR-related orphan receptorROR-γ293TLBDcastration-resistantprostatecancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
XY018
Cat. No.:
HY-120210
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.