CT1113
Based on 1 Customer Validation
CT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.61%
- No. CAS: 2523435-18-7
- Fòrmula: C25H29N5O2S
- Peso molecular:463.60
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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STAT5 |
BCR-ABL1 |
CT1113 (500 nM; 1-24 h) reduces c-MYC levels in various cancer cell lines within 1-2 h, decreases USP25, USP28, LSD1 and Tankyrase levels after 24 h, and enhances the ubiquitination of c-MYC and Tankyrase, without affecting the stability of p53 or CHK2[1].
CT1113 potently inhibits the proliferation of various tumor cell lines, with an EC50 of 65 nM in control HCT116 cells; its antiproliferative effect is largely targeted, as co-overexpression of USP25 and USP28 reduces the sensitivity of cells to CT1113[1].
CT1113 (0-600 nM; 72 h) potently inhibits the growth of human Ph+ALL cell lines, Ba/F3 cells expressing mutant BCR-ABL1, and primary Ph+ALL cells in vitro, with an IC50 of approximately 200 nM[2].
CT1113 (0-600 nM; 72 h) significantly induces apoptosis in human Ph+ALL cell lines, Ba/F3 cells expressing mutant BCR-ABL1, and primary Ph+ALL cells[2].
CT1113 (0-600 nM; 72 h) inhibits the phosphorylation of BCR-ABL1 and STAT5, and reduces the total protein levels of BCR-ABL1 and STAT5 in human Ph+ALL cell lines (this effect can be blocked by proteasome inhibition)[2].
CT1113 (0-600 nM; 72 h) enhances the ubiquitination level of BCR-ABL1, thereby promoting its proteasomal degradation in human Ph+ALL cell lines[2].
CT1113 (0-600 nM; 72 h) does not alter BCR-ABL1 mRNA levels in human Ph+ALL cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, HGC27, SMMC7721, diverse cancer cell lines
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Concentration:500 nM
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Incubation Time:24 h
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Result:Dramatically reduced c-MYC levels within 1-2 h across diverse cancer cell lines.\n
Dramatically decreased levels of USP25, USP28, LSD1, and Tankyrase after 24 h of treatment with 500 nM.\n
Increased ubiquitination of c-MYC and Tankyrase proteins.\nShowed no significant destabilization of p53 or CHK2 proteins.
CT1113 exhibits strong anti-tumor activity in a mouse colon cancer CDX model, significantly suppressing tumor growth[1].
CT1113(21 days) treatment of healthy C57BL/6 mice causes reversible mild body weight loss but no overt toxicity, does not disrupt intestinal crypt proliferation despite reducing overall intestinal c-MYC levels, and does not impair testicular tissue structure or spermatogonia proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2523435-18-7
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Appearance Solid
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Peso molecular 463.60
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Fòrmula C25H29N5O2S
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Color Light yellow to yellow
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SMILES
CNC1=C(C(N[C@@H]2CC3=CC=C(N4CC5NC(CC5)C4)C=C3OC2)=O)SC6=NC(C)=CC=C16
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (215.70 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: ≥ 5 mg/mL (10.79 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.79 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Pureza y Documentación
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Ficha de datos (275 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 2.1570 mL | 10.7852 mL | 21.5703 mL | 53.9258 mL |
| 5 mM | 0.4314 mL | 2.1570 mL | 4.3141 mL | 10.7852 mL | |
| 10 mM | 0.2157 mL | 1.0785 mL | 2.1570 mL | 5.3926 mL | |
| 15 mM | 0.1438 mL | 0.7190 mL | 1.4380 mL | 3.5951 mL | |
| 20 mM | 0.1079 mL | 0.5393 mL | 1.0785 mL | 2.6963 mL | |
| 25 mM | 0.0863 mL | 0.4314 mL | 0.8628 mL | 2.1570 mL | |
| 30 mM | 0.0719 mL | 0.3595 mL | 0.7190 mL | 1.7975 mL | |
| 40 mM | 0.0539 mL | 0.2696 mL | 0.5393 mL | 1.3481 mL | |
| 50 mM | 0.0431 mL | 0.2157 mL | 0.4314 mL | 1.0785 mL | |
| 60 mM | 0.0360 mL | 0.1798 mL | 0.3595 mL | 0.8988 mL | |
| 80 mM | 0.0270 mL | 0.1348 mL | 0.2696 mL | 0.6741 mL | |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2157 mL | 0.5393 mL |
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