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PRODUCT INFORMATION Floxuridine Item No. 14154

CAS Registry No.: 50-91-9 Formal Name: 2’-deoxy-5-fluoro-uridine H Synonyms: 5-FDU, 5-Fluorodeoxyuridine, N NSC 26740, NSC 27640 O O MF: C H FN O 9 11 2 5 O N FW: 246.2 HO F Purity: ≥98% Stability: ≥2 years at -20°C Supplied as: A crystalline solid HO UV/Vis.: λmax: 269 nm

Laboratory Procedures

For long term storage, we suggest that floxuridine be stored as supplied at -20°C. It should be stable for at least two years. Floxuridine is supplied as a crystalline solid. A stock solution may be made by dissolving the floxuridine in the solvent of choice. Floxuridine is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of floxuridine in these solvents is approximately 10 and 16 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of floxuridine can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of floxuridine in PBS, pH 7.2, is approximately 5 mg/ml. We do not recommend storing the aqueous solution for more than one day.

Description

Floxuridine is a prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid 1 injection. In addition, floxuridine inhibits thymidylate synthase (EC50 = 0.6 nM), interfering with DNA synthesis.2,3 It has been used to treat various cancers, particularly metastases to the liver.4

References

1. Ozawa, S., Hamada, M., Murayama, N., et al. Cytosolic and microsomal activation of doxifluridine and tegafur to produce 5-fluorouracil in human liver. Cancer Chemother. Pharmacol. 50, 454-458 (2002). 2. Ferguson, P.J., Collins, O., Dean, N.M., et al. Antisense down-regulation of thymidylate synthase to suppress growth and enhance cytotoxicity of 5-FUdR, 5-FU and Tomudex in HeLa cells. Br. J. Pharmacol. 127(8), 1777-1786 (1999). 3. Tzioumaki, N., Manta, S., Tsoukala, E., et al. Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: Novel 5-fluorouracil analogs that target thymidylate synthase. Eur. J. Med. Chem. 46(4), 993-1005 (2011). 4. Power, D.G. and Kemeny, N.E. The role of floxuridine in metastatic liver disease. Mol. Cancer Ther. 8(5), 1015-1025 (2009).

WARNING CAYMAN CHEMICAL THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD SAFETY DATA ANN ARBOR, MI 48108 · USA This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. PHONE: [800] 364-9897

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