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Floxuridine is an active metabolite of the fluorodeoxyuridylate (FdUMP) prodrug 5-fluorouracil (5-FU; Item No. 14416).1 It is formed from 5-FU by thymidine phosphorylase, which is then phosphorylated by thymidine kinase to form FdUMP. Floxuridine (1 µM) induces DNA double-strand breaks in thymidylate synthase-deficient FM3A murine breast cancer cells, as well as increases dATP levels and decreases dTTP and dGTP levels in FM3A F28-7 murine breast cancer cells expressing wild-type thymidylate synthase.2 It inhibits the proliferation of L1210 leukemia and HeLa cancer cells (IC50s = 1.1 and 9.4 nM, respectively).1 Floxuridine (200 mg/kg, i.p.) reduces tumor growth by 86.3% in a S180 murine sarcoma model.3 Formulations containing floxuridine have previously been used in the treatment of metastatic gastrointestinal adenocarcinoma.
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1. Synthesis and biological evaluation of unsaturated keto and exomethylene D-
2. Deoxyribonucleoside triphosphate imbalance. 5-
3. Tumor inhibitory effects of a new fluorouracil derivative: 5'-