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Fludarabine

Catalog No.
A5424
DNA synthsis inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$66.00
In stock
10mg
$59.00
In stock
50mg
$168.00
In stock
200mg
$330.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

Fludarabine (CAS 21679-14-1) is a purine analog prodrug that inhibits DNA synthesis. Upon cellular uptake, it undergoes phosphorylation to its active triphosphate form (F-ara-ATP), disrupting DNA replication through inhibition of critical enzymes such as DNA primase, DNA ligase I, ribonucleotide reductase, and DNA polymerases δ and ε. In human myeloma RPMI8226 cell assays, fludarabine suppressed cell growth, reduced Akt phosphorylation, and lowered anti-apoptotic proteins XIAP and Survivin. In vivo studies demonstrated marked tumor growth inhibition in RPMI8226 xenograft models. Fludarabine serves as a tool in oncology research, particularly leukemia and multiple myeloma-related studies.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt285.23
Cas No.21679-14-1
FormulaC10H12FN5O4
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 ConditionSmall 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.

Protocol

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

Applications

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.

Applications

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.

References:

[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

Fludarabine

Related Biological Data

Fludarabine

Related Biological Data

Fludarabine