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

Tezacitabine 

Cat. No.: HY-106014
Handling Instructions

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.

For research use only. We do not sell to patients.

Tezacitabine Chemical Structure

Tezacitabine Chemical Structure

CAS No. : 130306-02-4

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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].

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].

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.
Molecular Weight

257.22

Formula

C₁₀H₁₂FN₃O₄

CAS No.

130306-02-4

SMILES

F/C=C1[[email protected]](N2C(N=C(N)C=C2)=O)O[[email protected]](CO)[[email protected]]/1O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TezacitabineDNA/RNA SynthesisNucleoside Antimetabolite/AnalogApoptosisCytostaticcytotoxicantimetaboliteCytidinefluorineribonucleotide reductaseDNAreplicationrepairantitumorInhibitorinhibitorinhibit

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