GTSE1-IN-1
Based on 1 Customer Validation
GTSE1-IN-1 is an orally active GTSE1 inhibitor. GTSE1-IN-1 can suppress GTSE1 transcription and expression. GTSE1-IN-1 can inhibit cancer cell proliferation by inducing cell cycle arrest and cell senescence through the persistence of DNA damage. GTSE1-IN-1 can be used for the research of cancer, such as colon and lung cancer.
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- Purity : 98.07%
- CAS No.: 3002034-34-3
- 화학식: C21H24FN7
- 분자량:393.46
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보관:Powder -20°C, 3 years , 4°C, 2 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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용액&용해도
- 순도&문서
- References
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Help & FAQs
All DNA/RNA Synthesis Isoforms
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Biological Activity
제품 설명
In Vitro
GTSE1-IN-1 (Compound Y18) (0.5-2 μM, 48 h) inhibits the proliferation of HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 7 days) reduces the number of colony formation in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) induces G2/M phase arrest[1].
GTSE1-IN-1 (0.5-2 μM, 4 days) induces cell senescence in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) induces extensive DNA damage in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) reduces cell adhesion, migration and invasion in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) inhibits the transcription and protein expression of GTSE1 in HCT116 and A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and A549 cells
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Concentration:0.5, 1 and 2 μM
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Incubation Time:48 h
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Result:Increased cells in G2/M phase.
Decreased the expression of G2/M phase-related proteins cyclin B1 and CDC2.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116-derived xenograft tumor mice models[1]
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Dosage:15 and 30 mg/kg
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Administration:Intraperitoneally injection, every other day for 28 days
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Result:Reduced tumor volume.
Decreased the expression of GTSE1 and proliferation marker Ki67 in tumor tissues.
Increased the expression of DNA damage marker γ-H2AX.
Had no effect on body weight and liver/kidney function.
Chemical Information
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CAS No. 3002034-34-3
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Appearance Solid
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분자량 393.46
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화학식 C21H24FN7
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Color Off-white to light yellow
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SMILES
FC1=CN=C(NC2=CC=C(N3CCN(C)CC3)C=C2)N=C1NC4=CC=C(N)C=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (254.16 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
In Vivo Dissolution Calculator
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.
순도&문서
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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 | 2.5416 mL | 12.7078 mL | 25.4155 mL | 63.5389 mL |
| 5 mM | 0.5083 mL | 2.5416 mL | 5.0831 mL | 12.7078 mL | |
| 10 mM | 0.2542 mL | 1.2708 mL | 2.5416 mL | 6.3539 mL | |
| 15 mM | 0.1694 mL | 0.8472 mL | 1.6944 mL | 4.2359 mL | |
| 20 mM | 0.1271 mL | 0.6354 mL | 1.2708 mL | 3.1769 mL | |
| 25 mM | 0.1017 mL | 0.5083 mL | 1.0166 mL | 2.5416 mL | |
| 30 mM | 0.0847 mL | 0.4236 mL | 0.8472 mL | 2.1180 mL | |
| 40 mM | 0.0635 mL | 0.3177 mL | 0.6354 mL | 1.5885 mL | |
| 50 mM | 0.0508 mL | 0.2542 mL | 0.5083 mL | 1.2708 mL | |
| 60 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0590 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3177 mL | 0.7942 mL | |
| 100 mM | 0.0254 mL | 0.1271 mL | 0.2542 mL | 0.6354 mL |
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