Fludarabine triphosphate  (Synonyms: F-ara-ATP)

Fludarabine triphosphate (F-ara-ATP), the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC₅₀ of 2.3 μM and a K_i of 6.1 μM. Fludarabine triphosphate inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis^[1][2].

IC50: 2.3 ± 0.3 μM (DNA primase); Ki: 6.1 ± 0.3 μM (DNA primase)^[1]

Fludarabine triphosphate 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 (10-50 μM) inhibits the incorporation of ATP into primer RNA and dTTP into DNA to a similar extent^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

525.17

C₁₀H₁₅FN₅O₁₃P₃

74832-57-8

O[C@@H]([C@@H]1O)[C@](O[C@@H]1CO[P](O[P](O[P](O)(O)=O)(O)=O)(O)=O)([H])N2C3=NC(F)=NC(N)=C3N=C2

Room temperature in continental US; may vary elsewhere.

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

• [1]. Catapano CV, et al. Inhibition of primer RNA formation in CCRF-CEM leukemia cells by fludarabine triphosphate. Cancer Res. 1991 Apr 1;51(7):1829-35.  [Content Brief]

  [2]. Woodahl EL, et al. A novel phenotypic method to determine fludarabine triphosphate accumulation in T-lymphocytes from hematopoietic cell transplantation patients. Cancer Chemother Pharmacol. 2009 Feb;63(3):391-401.  [Content Brief]