Fludarabine triphosphate trisodium
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 591.12 |
| Molecular Formula | C10H12FN5Na3O13P3 |
| SMILES | O[C@@H]([C@@H]1O)[C@](O[C@@H]1CO[P](O[P](O[P](O)(O[Na])=O)(O[Na])=O)(O[Na])=O)([H])N2C3=NC(F)=NC(N)=C3N=C2 |
Summary
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 IC 50 of 2.3 μM and a K i 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] .
IC50 & Target
IC50: 2.3 ± 0.3 μM (DNA primase); Ki: 6.1 ± 0.3 μM (DNA primase) [1]
In Vitro
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]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
H 2 O : 125 mg/mL ( 211.46 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6917 mL | 8.4585 mL | 16.9170 mL |
| 5 mM | 0.3383 mL | 1.6917 mL | 3.3834 mL |
| 10 mM | 0.1692 mL | 0.8459 mL | 1.6917 mL |
References
- [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.
