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: 3094-09-5

Selleck's Doxifluridine has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.76%
99.76

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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 lnformation & 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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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