| ln Vitro |
GTx-027 (0.1–10,000 nM, 3 days) inhibited the proliferation of triple-negative breast cancer cells (such as MDA-MB-231 and HCC-38) in breast cancer cell proliferation assays [2]. GTx-027, as an androgen receptor (AR) agonist, activated AR in MDA-MB-231 cells in AR transcription activation assays [2]. GTx-027 (0.1–1,000 nM, 6 days) inhibited the proliferation of MDA-MB-231-AR cells in MDA-MB-231-AR cell proliferation assays [2]. GTx-027 (1 µM; 24 h) inhibited the migration and invasion of MDA-MB-231-AR:MSC co-culture cells in platypus migration assays and Transwell migration assays [2]. GTx-027 inhibited the expression of IL6 and MMP13 during co-culture in MDA-MB-231:MSC co-culture assays [2].
|
|---|---|
| ln Vivo |
GTx-027 (0.5-5 mg/kg; orally; for 28 days) increased pelvic floor muscle mass in ovariectomized mouse models [1]. GTx-027 (5-30 mg/kg; orally; three times a week; for 5 weeks) significantly inhibited tumor growth, reduced tumor weight, and had no obvious toxicity, and increased body weight in female nude mice with subcutaneous MDA-MB-231-AR cell xenograft tumors [2].
|
| Animal Protocol |
Animal/Disease Models:Female C57BL/6 mice (6–8 weeks old) underwent ovariectomy (OVX) or sham surgery [1].
Doses: 0.5 mg/kg, 2.5 mg/kg, 5 mg/kg Route of Administration: Oral administration; for 28 days Experimental Results: Pelvic floor muscle weight recovered to the level of the sham surgery group. Gene induction related to muscle catabolism was suppressed. Animal/Disease Models:MDA-MB-231-AR cells were subcutaneously implanted into female nude mice to establish a xenograft tumor model [2]. Doses: 5 mg/kg, 10 mg/kg, 30 mg/kg. Route of Administration: Oral administration, three times a week for 5 weeks. Experimental Results: Tumor growth inhibition rate exceeded 75%, and tumor weight was reduced by more than 50%. |
| References |
|
| Molecular Formula |
C18H14CLN3O3
|
|---|---|
| Molecular Weight |
355.78
|
| CAS # |
928122-40-1
|
| Appearance |
White to off-white solid
|
| SMILES |
N#CC(C=C1)=CC=C1OC[C@](C)(O)C(NC2=CC(Cl)=C(C=C2)C#N)=O
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~281.07 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2811 mL | 1.4054 mL | 2.8107 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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