GTx-027
Based on 1 Customer Validation
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.
- Purity: 99.61%
- CAS No.: 928122-40-1
- Formula: C18H14ClN3O3
- Molecular Weight:355.78
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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.
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Cell Line:MDA-MB-231, HCC-38
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:3 days
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Result:Reduced the proliferation of these cells compared to vehicle-treated cells.
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Cell Line:MDA-MB-231-AR
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:6 days
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Result:Inhibited the proliferation of MDA-MB-231-AR cells.
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Cell Line:MDA-MB-231-AR
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Concentration:1 µM
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Incubation Time:24 hrs
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Result:Inhibited the migration of cells.
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.
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Animal Model:Female C57BL/6 mice (6-8 weeks old) were ovariectomized (OVX) or sham operated[1].
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Dosage:0.5 mg/kg, 2.5 mg/kg, 5 mg/kg
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Administration:p.o.; for 28 days
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Result:Resulted in a restoration of the pelvic muscles to the sham-operated weight.
The induction of genes associated with muscle catabolism was inhibited.
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Animal Model:Female nude mice were subcutaneously implanted with MDA-MB-231-AR cells to establish the xenograft tumor model[2].
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Dosage:5 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration, three times a week, for 5 weeks
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Result:Resulting in greater than 75% tumor growth inhibition and more than 50% tumor weight reduction.
Chemical Information
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CAS No. 928122-40-1
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Appearance Solid
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Molecular Weight 355.78
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Formula C18H14ClN3O3
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Color White to off-white
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SMILES
N#CC(C=C1)=CC=C1OC[C@](C)(O)C(NC2=CC(Cl)=C(C=C2)C#N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Suriyan Ponnusamy, et al. Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice. J Cell Biochem. 2017 Mar;118(3):640-646. [Content Brief]
[2]. Narayanan R, et al. Selective androgen receptor modulators (SARMs) negatively regulate triple-negative breast cancer growth and epithelial:mesenchymal stem cell signaling. PLoS One. 2014 Jul 29;9(7):e103202. [Content Brief]
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 |
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