For research use only. Not for therapeutic Use.
Fludarabine triphosphate (F-ara-ATP) trisodium, 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 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].
| Catalog Number | I042844 |
| Synonyms | trisodium;[[[(2R,3S,4S,5R)-5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] hydrogen phosphate |
| Molecular Formula | C10H12FN5Na3O13P3 |
| Purity | ≥95% |
| InChI | InChI=1S/C10H15FN5O13P3.3Na/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(18)5(17)3(27-9)1-26-31(22,23)29-32(24,25)28-30(19,20)21;;;/h2-3,5-6,9,17-18H,1H2,(H,22,23)(H,24,25)(H2,12,14,15)(H2,19,20,21);;;/q;3*+1/p-3/t3-,5-,6+,9-;;;/m1.../s1 |
| InChIKey | ABCNYMXTKKBAHQ-ABDPYLPCSA-K |
| SMILES | C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)COP(=O)([O-])OP(=O)([O-])OP(=O)(O)[O-])O)O)F)N.[Na+].[Na+].[Na+] |
| Reference | [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. [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. |
