2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis
  4. Tezacitabine

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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Tezacitabine Chemical Structure

Tezacitabine Chemical Structure

CAS No. : 130306-02-4

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5 mg USD 970 In-stock
10 mg USD 1550 In-stock
25 mg USD 3080 In-stock
50 mg USD 4900 In-stock
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Based on 1 publication(s) in Google Scholar

Tezacitabine Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

Ribonucleotide reductase[1]
In Vitro

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.

Tezacitabine Related Antibodies

Cell Cycle Analysis[1]

Cell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
Concentration: 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM
Incubation Time: 24 hours
Result: Induced the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) leaky block of the cell cycle.

Apoptosis Analysis[1]

Cell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
Concentration: 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM
Incubation Time: 24 hours
Result: Induced apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.
In Vivo

Tezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits tumor growth in HCT 116 tumor xenografts[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (7-9-week-old) injected with HCT 116 cells[2]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; daily; 14 days
Result: Inhibited tumor growth in HCT 116 tumor xenografts.
Clinical Trial
Molecular Weight

257.22

Formula

C10H12FN3O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

F/C=C1[C@H](N2C(N=C(N)C=C2)=O)O[C@H](CO)[C@H]/1O
Shipping

Shipping with dry ice.
Storage

-80°C
Solvent & Solubility
In Vitro: 

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 : 200 mg/mL (777.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8877 mL 19.4386 mL 38.8772 mL
5 mM 0.7775 mL 3.8877 mL 7.7754 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (388.77 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.35%

COA (248 KB) HNMR (176 KB) RP-HPLC (194 KB) LCMS (93 KB)

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. When stored at -80°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 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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Tezacitabine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tezacitabine130306-02-4DNA/RNA SynthesisNucleoside Antimetabolite/AnalogApoptosisCytostaticcytotoxicantimetaboliteCytidinefluorineribonucleotide reductaseDNAreplicationrepairantitumorInhibitorinhibitorinhibit

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