| Name | Doxifluridine |
| Description | Doxifluridine (AMC 0101) is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand. |
| In vitro | Doxifluridine suppresses tube formation of HUVEC and vascular endothelial growth factor production by FU-MMT-1 cells. [1] Doxifluridine is converted to 5-FU and subsequently to FdUMP, and the results suggest that Doxifluridine exerts its cytotoxic effects through inhibition of TS and incorporation into RNA. [2] Doxifluridine is a fluoropyrimidine derivative that is activated preferentially in malignant cells by thymidine phosphorylase to form 5-fluorouracil (5-FU). Doxifluridine is developed to improve the therapeutic index of 5-FU and to reduce toxicity, including the immunosuppressive, myelosuppressive, and cardiotoxic effects of 5-FU and other fluorinated pyrimidines. [3] |
| In vivo | Metronomic Doxifluridine alone significantly suppresses tumor growth compared with the untreated (control) group, while metronomic Doxifluridine in combination with TNP-470 significantly inhibits tumor growth compared with each treatment alone in in FU-MMT-1 xenografts. Doxifluridine in combination with TNP-470 also leads to a significant reduction of intratumoral vascularity. [1] Doxifluridine significantly inhibits the growth of KPL-4 tumors, reduces the tissue levels of IL-6, and alleviates body weight loss in nude mice bearing KPL-4 tumors. [4] Doxifluridine results in a significant reduction in the activity of phenytoin p-hydroxylation in rats. Doxifluridine decreases the elimination rate constant and the total clearance in rats. [5] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 45 mg/mL (182.8 mM)
DMSO : 55 mg/mL (223.4 mM)
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| Keywords | Nucleoside Antimetabolite/Analog | Inhibitor | AMC-0101 | Doxifluridine | AMC0101 | inhibit |
| Inhibitors Related | Stavudine | Rifampicin | 5-Fluorouracil | Procaine | Ribavirin | Guanidine hydrochloride | 2,4-D | N-Nitrosodiethylamine | Acyclovir | Thymidine | Temozolomide | Folic acid |
| Related Compound Libraries | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
