IC50: 2.3 ± 0.3 μM (DNA primase); Ki: 6.1 ± 0.3 μM (DNA primase)[1]
Fludarabine triphosphate (F-ara-ATP) trisodium, the active metabolite of Fludarabine , is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate trisodium inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate trisodium inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis[1][2].
Fludarabine triphosphate trisodium is a more potent inhibitor of the polydeoxythymidylate primase activity than of the DNA polymerase α/δ activities present in the supernatants of CCRF-CEM cells[1].
Fludarabine triphosphate trisodium (10-50 μM) inhibits the incorporation of ATP into primer RNA and dTTP into DNA to a similar extent[1].