Home Metabolism Phosphorylase activator Doxifluridine For research use only.

Doxifluridine

Synonyms: 5'-DFUR, AMC 0101

Doxifluridine (5'-DFUR, AMC 0101) is an oral prodrug that is converted to the cytotoxic agent 5-fluorouracil (5-FU).

Doxifluridine Chemical Structure

Doxifluridine Chemical Structure

CAS No. 3094-09-5

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Doxifluridine Related Products

Biological Activity

Description Doxifluridine (5'-DFUR, AMC 0101) is an oral prodrug that is converted to the cytotoxic agent 5-fluorouracil (5-FU).
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00662025 Completed
Advanced/Metastatic Breast Cancer
Pfizer
 April 2008 Phase 2
NCT00532948 Completed
Glioma
Hoffmann-La Roche
 May 2007 Phase 1
NCT00353262 Completed
Colorectal Cancer
Hoffmann-La Roche
 July 2005 Phase 1

Chemical Information & Solubility

Molecular Weight 246.19 Formula

C9H11FN2O5
CAS No. 3094-09-5 SDF Download Doxifluridine SDF
Smiles CC1C(C(C(O1)N2C=C(C(=O)NC2=O)F)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (199.03 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 49 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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