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- Fludarabine Phosphate (Fludara)
Fludarabine Phosphate (Fludara)
Fludarabine phosphate is a STAT-1 activation inhibitor and a DNA synthesis inhibitor. Fludarabine 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.
- 1. Wenli Yuan, Deyao Deng, et al. "IFNγ/PD-L1 Signaling Improves the Responsiveness of Anti-PD-1 Therapy in Colorectal Cancer: An in vitro Study." Onco Targets Ther. 2021 May 7;14:3051-3062. PMID:33994797
- 2. Diqi Yang, Ai Liu, et al. "BCL2L15 Depletion Inhibits Endometrial Receptivity via the STAT1 Signaling Pathway." Genes (Basel). 2020 Jul 17;11(7):816. PMID:32708974
- 3. Deng R, Zhang P, et al. "HDAC is indispensable for IFN-γ-induced B7-H1 expression in gastric cancer." Clin Epigenetics. 2018 Dec 11;10(1):153. PMID:30537988
- 4. Yuan W, Deng D,et al."Hyperresponsiveness to interferon gamma exposure as a response mechanism to anti-PD-1 therapy in microsatellite instability colorectal cancer." Cancer Immunol Immunother. 2018 Nov 7. PMID:30406373
| Storage | Store at -20°C |
| M.Wt | 365.21 |
| Cas No. | 75607-67-9 |
| Formula | C10H13FN5O7P |
| Synonyms | Fludura |
| Solubility | insoluble in EtOH; ≥17.6 mg/mL in DMSO; ≥6.7 mg/mL in H2O with gentle warming and ultrasonic |
| Chemical Name | [(2R,3S,4S,5R)-5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate |
| SDF | Download SDF |
| Canonical SMILES | C1=NC2=C(N1C3C(C(C(O3)COP(=O)(O)O)O)O)N=C(N=C2N)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Human T lymphoblastoid cells, CCRF-CEM |
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Reaction Conditions |
0.3 ~ 100 μM fludarabine phosphate for 5 h incubation |
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Applications |
Fludarabine phosphate (0.3 ~ 100 μM) was dose-dependently converted to F-ara-ATP in cells. However, the incorporation of F-ara-ATP into DNA was self-limited. At 0.3 ~ 10 μM fludarabine phosphate, the amount of the F-ara-AMP incorporated into DNA increased in a dose-dependent manner, but could not further increased at fludarabine phosphate concentrations greater than 10 μM. |
| Animal experiment:[2] | |
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Animal models |
Mice bearing P388 leukemia |
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Dosage form |
234 mg/kg Injected intraperitoneally |
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Applications |
Fludarabine phosphate administered as a single dose resulted in fewer cells surviving therapy in mice bearing P388 leukemia, accompanied by a greater percentage of increase in life span (110%) and increased median survival time. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Huang P, Chubb S, Plunkett W. Termination of DNA synthesis by 9-beta-D-arabinofuranosyl-2-fluoroadenine. A mechanism for cytotoxicity. Journal of Biological Chemistry, 1990, 265(27): 16617-16625. 2. Avramis VI, Plunkett W. Metabolism and therapeutic efficacy of 9-beta-D-arabinofuranosyl-2-fluoroadenine against murine leukemia P388. Cancer Research, 1982, 42(7): 2587-2591. |
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| Description | Fludarabine is an inhibitor of STAT1 activation and a DNA synthesis. | |||||
| Targets | DNA synthesis | |||||
| IC50 | ||||||
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