Tezacitabine

Modify Date: 2024-01-04 10:50:22

Tezacitabine Structure
Tezacitabine structure
Common Name Tezacitabine
CAS Number 130306-02-4 Molecular Weight 275.234
Density N/A Boiling Point 590.1ºC at 760 mmHg
Molecular Formula C10H12FN3O4 Melting Point N/A
MSDS N/A Flash Point 310.7ºC

 Use of 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[1][2].

 Names

Name 4-amino-1-[(2R,3E,4S,5R)-3-(fluoromethylidene)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
Synonym More Synonyms

 Tezacitabine Biological Activity

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].
Related Catalog
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.
References

[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.

[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.

 Chemical & Physical Properties

Boiling Point 590.1ºC at 760 mmHg
Molecular Formula C10H12FN3O4
Molecular Weight 275.234
Flash Point 310.7ºC
Exact Mass 275.091736
PSA 110.60000

 Synonyms

MDL 101,731
tezaciabine
FMdC
tezacitabine
2'-Deoxy-2'-(fluoromethylene)cytidine hydrate (1:1)
Fmdc cpd
Cytidine, 2'-deoxy-2'-(fluoromethylene)-, hydrate (1:1)
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