Biocaxis > Products > Nucleoside |
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Fludarabine
Catalog NO.: NS-002
| CAS NO.: 21679-14-1 |
Brand: BIOCAXIS
Category
Nucleosides & Nucleotides, nucleobase
Synonyms:
9-β-D-Arabinofuranosyl-2-fluoroadenine, F-ara-A, Fludarabine des-phosphate
2-F-Ara-Ar; 2-Fluoro-arabinoadenosine; 9-(β-D-Arabinofuranosyl)-2-fluoroadenine; F-ara-A;
NSC 118218;
(2R,3S,4S,5R)-2-(6-Amino-2-fluoro-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol;
2-fluoro-9-β-D-arabinofuranosyladenine
Molecular Formula
C10H12FN5O4
Molecular Weight
285.23
General description
Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a
fluorinated purine analogue with antineoplastic activity in lymphoproliferative
malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and
STAT1-dependent gene transcription in normal resting or activated lymphocytes.
2-Fluoroadenine-9-β-D-arabinofuranoside
(F-ara-A) has been used:
to assess its interaction with kinase inhibitor UCN-01 in
human leukemia cells (U937 and HL-60) and primary patient samples
to assess its influence on endothelial cells by apoptosis
assay and human microvascular endothelial cells (HMECs) by cytotoxicity assay
in comparative cytotoxicity studies with Alemtuzumab CDC in
17p13- chronic lymphocytic leukemia (CLL) patients
Biochem/physiol Actions
Fludarabine (the 5′-phosphate) is a prodrug that is
converted to F-ara-A, which enters cells and
accumulates primarily as the 5′-triphosphate. F-ara-A
interferes with DNA synthesis and repair and induces apoptosis of cancer cells.
Fludarabine (the 5′-phosphate) is a prodrug that is
converted to F-ara-A, which enters cells and
accumulates primarily as the 5′-triphosphate. F-ara-A
interferes with DNA synthesis and repair and induces apoptosis of cancer cells.
F-ara-A also strongly inhibits DNA methylation,
particularly methylation of cytosine in CpG dinucleotide sequences.
Biochem/physiol Actions
5-Azacytidine (Aza-CR) acts as a potential chemotherapeutic
regimen for acute myelogenous leukemia. This drug has an ability to selectively
increase γ-globin synthesis. Therefore, 5-azacytidine is used in treating
severe β-thalassemia. Aza-CR acts as a potential bacteriostatic, antitumor
and mutagenic agent. In addition, it also exhibits various biological activity
such as, immunosuppressive, antimitotic, radioprotective and virostatic effects.
A potent growth inhibitor and cytotoxic agent; inhibits DNA
methyltransferase, an important regulatory mechanism of gene expression, gene
activation and silencing.
Causes DNA demethylation or hemi-demethylation, creating
openings that allow transcription factors to bind to DNA and reactivate tumor
suppressor genes.
Potent growth inhibitor and cytotoxic agent; inhibits DNA
methyltransferase.