TAS1553
Based on 1 publication(s) in Google Scholar
TAS1553 is a potent, orally active protein-protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.50%
- CAS. Nr.: 2166023-31-8
- Formel: C20H20ClFN4O5S
- Molecular Weight:482.91
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TAS1553
More
Biologische Aktivität
Beschreibung
In Vitro
TAS1553 (0.001-1 μM) inhibits the enzymatic activity of RNR in a dose-dependent manner[1].
TAS1553 (3 d) has anti-proliferative activity against both solid and hematological human cancer cell lines and the GI50 values ranged from 0.228 to 4.15 μM[1].
TAS1553 (1-10 μM; 0-2 h; HCC38 and MV-4-11 cells) reduces intracellular dATP pool in a dose- and time-dependent manner, which is a critical metabolite for DNA replication[1].
TAS1553 (0-10 μM; 0-24 h; HCC38 and MV-4-11 cells) induces the replication stress and apoptosis in a dose- and time-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC38 and MV-4-11 cells
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Concentration:0, 0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:0, 1, 2, 4, 8 and 24 hours
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Result:Increased the expression of Ser345, Ser4, Ser8 and Thr21 phosphorylation. Increaed the levels cleaved PARP and cleaved caspase-3.
In Vivo
TAS1553 (50-200 mg/kg; p.o.; daily, for 15 d; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) has antitumor activity in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice[1]
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Dosage:25, 50, 100 and 200 mg/kg
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Administration:Oral administration; for 24hours
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Result:Reduces intracellular dATP pool and induces the replication stress and apoptosis.
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Animal Model:Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice[1]
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Dosage:50, 100 and 200 mg/kg
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Administration:Oral administration; daily, for 15 days
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Result:Inhibited tumor growth in the treated group/control group (T/C) were 52.0 (50 mg/kg), 45.0 (100 mg/kg) and 29.4% (200 mg/kg), respectively.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- Pull-down
- Immunoprecipitation
- Protocol for Bimolecular Fluorescence Complementation (BiFC) Assay
- Apoptosis Solutions
- Co-Immunoprecipitation
- Protocol for Yeast Two-Hybrid (Y2H) Assay
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2166023-31-8
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Appearance Solid
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Molecular Weight 482.91
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Formel C20H20ClFN4O5S
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Color White to off-white
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SMILES
O=C(N)C1=CC(Cl)=CC=C1S(=O)(N[C@H](C(O2)=NNC2=O)[C@@H](C3=C(C)C(C)=CC=C3F)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (207.08 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.18 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.
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.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.0708 mL | 10.3539 mL | 20.7078 mL | 51.7695 mL |
| 5 mM | 0.4142 mL | 2.0708 mL | 4.1416 mL | 10.3539 mL | |
| 10 mM | 0.2071 mL | 1.0354 mL | 2.0708 mL | 5.1769 mL | |
| 15 mM | 0.1381 mL | 0.6903 mL | 1.3805 mL | 3.4513 mL | |
| 20 mM | 0.1035 mL | 0.5177 mL | 1.0354 mL | 2.5885 mL | |
| 25 mM | 0.0828 mL | 0.4142 mL | 0.8283 mL | 2.0708 mL | |
| 30 mM | 0.0690 mL | 0.3451 mL | 0.6903 mL | 1.7256 mL | |
| 40 mM | 0.0518 mL | 0.2588 mL | 0.5177 mL | 1.2942 mL | |
| 50 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0354 mL | |
| 60 mM | 0.0345 mL | 0.1726 mL | 0.3451 mL | 0.8628 mL | |
| 80 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6471 mL | |
| 100 mM | 0.0207 mL | 0.1035 mL | 0.2071 mL | 0.5177 mL |
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