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Catalog No.
DNA synthsis inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock
In stock
In stock

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Fludarabine is a purine analog that inhibits DNA synthesis [1].

DNA synthesis is a natural creation of deoxyribonucleic acid (DNA) molecules and plays an important role in cell growth.

Fludarabine is a prodrug and is phosphorylated to the nucleoside triphosphate (F-ara-ATP) in cells to elicit biological activity. It affected a series of enzymes that required in DNA synthesis such as DNA primase, DNA polymerases, DNA ligase I, ribonucleotide reductase and 3’-5’ exonuclease activity of DNA polymerases δ and ε [1]. In human myeloma cell RPMI8226, fludarabine significantly inhibited cells growth and reduced phosphorylation of Akt. Also, it reduced XIAP and survivin, the inhibitors of apoptosis proteins (IAP) family [2]. Fludarabine can act as a cytosolic 50-nucleotidase II (cN-II) inhibitor [3].

In immunodeficient mice bearing RPMI8226 myeloma xenografts, fludarabine (40 mg/kg) slowed down the growth of tumors by about 5-fold in 25 d comparing with the control tumors [2].

[1].  Gandhi V, Huang P, Plunkett W. Fludarabine inhibits DNA replication: a rationale for its use in the treatment of acute leukemias. Leuk Lymphoma, 1994, 14 Suppl 2: 3-9.
[2].  Meng H, Yang C, Ni W, et al. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo. Eur J Haematol, 2007, 79(6): 486-493.
[3].  Cividini F, Pesi R, Chaloin L, et al. The purine analog fludarabine acts as a cytosolic 5'-nucleotidase II inhibitor. Biochem Pharmacol, 2015, 94(2): 63-68.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.21679-14-1
Solubilityinsoluble in H2O; insoluble in EtOH; ≥9.25 mg/mL in DMSO
Chemical Name(2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
SDFDownload SDF
Canonical SMILESC1=NC2=C(N1C3C(C(C(O3)CO)O)O)N=C(N=C2N)F
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.


Cell experiment [1]:

Cell lines

RPMI 8226 cells

Preparation method

The solubility of this compound in DMSO is > 9.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1, 2 or 4 μg/mL; 6, 12 or 24 hrs


Fludarabine potently inhibited the proliferation of RPMI 8226 cells in dose- and time-dependent manners, with an IC50 value of 1.54 μg/mL. Fludarabine arrested RPMI 8226 cells in the G1 phase of cell cycle and triggered apoptosis. The immunoblotting results showed that Fludarabine time-dependently induced cleavage of caspase-8, -9, -3 and -7, followed by PARP cleavage. In addition, Fludarabine time-dependently up-regulated Bax expression, without affecting Bak expression.

Animal experiment [1]:

Animal models

SCID mice bearing RPMI 8226 cells

Dosage form

40 mg/kg; i.p.


Tumors of mice treated with PBS grew rapidly, to approximately 10 folds of their initial volume in the 25th day, whereas, tumors in the Fludarabine treatment group increased less than 5 folds. In SCID mice bearing RPMI 8226 cells, treatment with 40 mg/kg Fludarabine for 10 days resulted in a significant increase in the number of apoptotic cells.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1]. Meng H, Yang C, Ni W, et al. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo. Eur J Haematol, 2007, 79(6): 486-493.

Quality Control

Chemical structure


Related Biological Data


Related Biological Data