Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
4.0619 mL
20.3095 mL
40.6190 mL
5 mM
0.8124 mL
4.0619 mL
8.1238 mL
10 mM
0.4062 mL
2.0310 mL
4.0619 mL
50 mM
0.0812 mL
0.4062 mL
0.8124 mL
Description
Doxifluridine (5'-DFUR, AMC 0101) is an oral prodrug that is converted to the cytotoxic agent 5-fluorouracil (5-FU).
In vitro
Doxifluridine suppresses tube formation of HUVEC and vascular endothelial growth factor production by FU-MMT-1 cells. 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. 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.
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. 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. 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.
