fludarabine triphosphate

Fludarabine triphosphate (F-ara-ATP), the cytotoxic metabolite of Fludarabine phosphate, inhibits ribonucleotide reductase and DNA polymerase, ultimately leading to cellular apoptosis.

Fludarabine triphosphate (F-ara-ATP) trisodium, the principal metabolite of Fludarabine, is a potent, noncompetitive, and specific inhibitor of DNA primase with an IC50 value of 2.3 μM and a Ki of 6.1 μM. It obstructs DNA synthesis by hindering DNA primase and primer RNA formation, while also inhibiting ribonucleotide reductase and DNA polymerase activities, effectively inducing cellular apoptosis [1] [2].

Fludarabine Phosphate (NSC 312887 Phosphate) is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.