(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE

257.22

257.22

7607Y95N9S

DTXSID10156446

C95916

Off-white to light yellow

110.60000

-0.48930

1.71±0.1 g/cm3(Predicted)

512.5±60.0 °C(Predicted)

310.7ºC

12.50±0.60(Predicted)

-80°C

Investigated for use/treatment in colorectal cancer, lung cancer, leukemia (unspecified), and gastric cancer.

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. (See all compounds classified as Enzyme Inhibitors.)|Drugs used to potentiate the effectiveness of radiation therapy in destroying unwanted cells. (See all compounds classified as Radiation-Sensitizing Agents.)

Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types.

2'-deoxy-2'-(fluoromethylene)cytidine