Tezacitabine
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Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.
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- Pureté: 99.97%
- CAS No.: 130306-02-4
- Formule: C10H12FN3O4
- Masse moléculaire:257.22
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Stockage:
-80°C
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Ribonucleotide reductase[1]
Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment induces the G1 and S-phase leaky block of the cell cycle[1].
Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner[1].
Tezacitabine has strong cytostatic and cytotoxic properties. Cytotoxic effect of Tezacitabine reveals not only as apoptosis, but also as a change in protein metabolism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
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Concentration:0.01 µM, 0.1 µM, 1.0 µM, and 10 µM
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Incubation Time:24 hours
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Result:Induced the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) leaky block of the cell cycle.
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Cell Line:CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
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Concentration:0.01 µM, 0.1 µM, 1.0 µM, and 10 µM
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Incubation Time:24 hours
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Result:Induced apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (7-9-week-old) injected with HCT 116 cells[2]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection; daily; 14 days
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Result:Inhibited tumor growth in HCT 116 tumor xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 130306-02-4
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Appearance Solid
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Masse moléculaire 257.22
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Formule C10H12FN3O4
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Color Off-white to light yellow
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SMILES
F/C=C1[C@H](N2C(N=C(N)C=C2)=O)O[C@H](CO)[C@H]/1O
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Livraison
Shipping with dry ice.
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Stockage
-80°C
Solvant et solubilité
DMSO : 200 mg/mL (777.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (388.77 mM; Need ultrasonic)
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. When stored at -80°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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. When stored at -80°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (19.44 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 (19.44 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (388.77 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
[1]. Janusz S Skierski, et al. Tezacitabine Blocks Tumor Cells in G1 and S Phases of the Cell Cycle and Induces Apoptotic Cell Death. Acta Pol Pharm. May-Jun 2005;62(3):195-205. [Content Brief]
[2]. Pietro Taverna, et al. Tezacitabine Enhances the DNA-directed Effects of Fluoropyrimidines in Human Colon Cancer Cells and Tumor Xenografts. Biochem Pharmacol. 2007 Jan 1;73(1):44-55. [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. When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.8877 mL | 19.4386 mL | 38.8772 mL | 97.1931 mL |
| 5 mM | 0.7775 mL | 3.8877 mL | 7.7754 mL | 19.4386 mL | |
| 10 mM | 0.3888 mL | 1.9439 mL | 3.8877 mL | 9.7193 mL | |
| 15 mM | 0.2592 mL | 1.2959 mL | 2.5918 mL | 6.4795 mL | |
| 20 mM | 0.1944 mL | 0.9719 mL | 1.9439 mL | 4.8597 mL | |
| 25 mM | 0.1555 mL | 0.7775 mL | 1.5551 mL | 3.8877 mL | |
| 30 mM | 0.1296 mL | 0.6480 mL | 1.2959 mL | 3.2398 mL | |
| 40 mM | 0.0972 mL | 0.4860 mL | 0.9719 mL | 2.4298 mL | |
| 50 mM | 0.0778 mL | 0.3888 mL | 0.7775 mL | 1.9439 mL | |
| 60 mM | 0.0648 mL | 0.3240 mL | 0.6480 mL | 1.6199 mL | |
| 80 mM | 0.0486 mL | 0.2430 mL | 0.4860 mL | 1.2149 mL | |
| 100 mM | 0.0389 mL | 0.1944 mL | 0.3888 mL | 0.9719 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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