2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. GTx-027

GTx-027 is an orally active and non-steroidal selective androgen receptor modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI).

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

GTx-027 Chemical Structure

GTx-027 Chemical Structure

CAS No. : 928122-40-1

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg 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

GTx-027 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GTx-027 is an orally active and non-steroidal selective androgen receptor modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI)[1][2].

In Vitro

GTx-027 (0.1-10000 nM, 3 days) inhibits the proliferation of triple-negative breast cancer cells such as MDA-MB-231 and HCC-38 in the breast cancer cell proliferation assay[2].
GTx-027 acts as an AR agonist and activates AR in MDA-MB-231 cells in the AR transactivation assay[2].
GTx-027 (0.1-1000 nM, 6 days) inhibits the proliferation of MDA-MB-231-AR cells in the MDA-MB-231-AR cell proliferation assay[2].
GTx-027 (1 µM; 24 h) inhibits the migration and invasion of MDA-MB-231-AR:MSC co-cultured cells in the Platypus migration assay and Transwell migration assay[2].
GTx-027 inhibits the expression of IL6 and MMP13 during the co-culture in the MDA-MB-231:MSC co-culture experiment[2].

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

GTx-027 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: MDA-MB-231, HCC-38
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 3 days
Result: Reduced the proliferation of these cells compared to vehicle-treated cells.

Cell Proliferation Assay[2]

Cell Line: MDA-MB-231-AR
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 6 days
Result: Inhibited the proliferation of MDA-MB-231-AR cells.

Cell Migration Assay [2]

Cell Line: MDA-MB-231-AR
Concentration: 1 µM
Incubation Time: 24 hrs
Result: Inhibited the migration of cells.
In Vivo

GTx-027 (0.5-5 mg/kg; p.o.; for 28 days) results in an increase in pelvic floor muscles in an ovariectomized mouse model[1].
GTx-027 (5-30 mg/kg; oral administration; three times a week; 5 weeks) significantly inhibits tumor growth, reduces tumor weight, shows no obvious toxicity, and increases the body weight of animals in the subcutaneous xenograft tumor model of MDA-MB-231-AR cells in female nude mice[2].

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

Animal Model: Female C57BL/6 mice (6-8 weeks old) were ovariectomized (OVX) or sham operated[1].
Dosage: 0.5 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration: p.o.; for 28 days
Result: Resulted in a restoration of the pelvic muscles to the sham-operated weight.
The induction of genes associated with muscle catabolism was inhibited.
Animal Model: Female nude mice were subcutaneously implanted with MDA-MB-231-AR cells to establish the xenograft tumor model[2].
Dosage: 5 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration, three times a week, for 5 weeks
Result: Resulting in greater than 75% tumor growth inhibition and more than 50% tumor weight reduction.
Molecular Weight

355.78

Formula

C18H14ClN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC(C=C1)=CC=C1OC[C@](C)(O)C(NC2=CC(Cl)=C(C=C2)C#N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (281.07 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 2.8107 mL 14.0536 mL 28.1073 mL
5 mM 0.5621 mL 2.8107 mL 5.6215 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.03 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (7.03 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8107 mL 14.0536 mL 28.1073 mL 70.2681 mL
5 mM 0.5621 mL 2.8107 mL 5.6215 mL 14.0536 mL
10 mM 0.2811 mL 1.4054 mL 2.8107 mL 7.0268 mL
15 mM 0.1874 mL 0.9369 mL 1.8738 mL 4.6845 mL
20 mM 0.1405 mL 0.7027 mL 1.4054 mL 3.5134 mL
25 mM 0.1124 mL 0.5621 mL 1.1243 mL 2.8107 mL
30 mM 0.0937 mL 0.4685 mL 0.9369 mL 2.3423 mL
40 mM 0.0703 mL 0.3513 mL 0.7027 mL 1.7567 mL
50 mM 0.0562 mL 0.2811 mL 0.5621 mL 1.4054 mL
60 mM 0.0468 mL 0.2342 mL 0.4685 mL 1.1711 mL
80 mM 0.0351 mL 0.1757 mL 0.3513 mL 0.8784 mL
100 mM 0.0281 mL 0.1405 mL 0.2811 mL 0.7027 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.

GTx-027 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:

GTx-027928122-40-1GTx027GTx 027Androgen Receptororally activeselective androgen receptor modulatorSARMstress urinary incontinence (SUI)breast cancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GTx-027
Cat. No.:
HY-171048
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 (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

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