Cat. No. Name Size Price Add Cart
KI0716Floxuridine50 mg$154
Floxuridine200 mg$432

Chemical Characteristic

Product NameFloxuridine
Synonyms5-fluorodeoxyuridine, FUDR
CAS No.50-91-9
Molecular Weight 246.19
FormulaC9H11FN2O5
Chemical Structure

Biological activities

Floxuridine is a prodrug form of 5-fluorouracil (5-FU). Floxuridine is a fluorinated pyrimidine antimetabolite. Floxuridine is most often used in the treatment of colorectal cancer. [1] Floxuridine exhibits oligopeptide transporter 1 (PEPT1) affinity and inhibits Gly-Sar uptake with IC50 of 7.3 and 6.3 mM in Caco-2 and AsPC-1 cells, respectively. Floxuridine shows a 12-fold higher Caco-2 membrane permeability than 5-FU. [2] Floxuridine inhibits cell growth with GI50 of 17.6 and 22.9 mM in Capan-2 and AsPC-1 cells, respectively. [3] In vivo, floxuridine is a specific substrate of thymidine phosphorylase. [4]

References

[1] Ludwig J, et al. Floxuridine-induced sclerosing cholangitis: an ischemic cholangiopathy? Hepatology. 1989, 9(2): 215-218. 閵嗏偓閵嗏偓
[2] Tsume Y, et al. Enhanced absorption and growth inhibition with amino acid monoester prodrugs of floxuridine by targeting hPEPT1 transporters. Molecules. 2008, 13(7): 1441-1454. 閵嗏偓閵嗏偓
[3] Tsume Y, et al. Enhanced cancer cell growth inhibition by dipeptide prodrugs of floxuridine: increased transporter affinity and metabolic stability. Mol Pharm. 2008, 5(5): 717-727. 閵嗏偓閵嗏偓
[4] Yagil E, et al. Phosphorolysis of 5-fluoro-2'-deoxyuridine in Escherichia coli and its inhibition by nucleosides. J Bacteriol. 1971, 108(2): 760-764. 閵嗏偓閵嗏偓閵嗏偓

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