Doxifluridine

Catalog No.S2045 Synonyms: 5'-DFUR, AMC 0101

For research use only.

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

Doxifluridine Chemical Structure

CAS No. 3094-09-5

Selleck's Doxifluridine has been cited by 3 Publications

Purity & Quality Control

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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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 49 mg/mL
(199.03 mM)
Water 49 mg/mL
(199.03 mM)
Ethanol Insoluble

Chemical Information

Molecular Weight 246.19
Formula

C9H11FN2O5

CAS No. 3094-09-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C(C(C(O1)N2C=C(C(=O)NC2=O)F)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01199250 Not yet recruiting Other: Laboratory Biomarker Analysis Lynch Syndrome|Recurrent Uterine Corpus Carcinoma|Stage I Uterine Corpus Cancer|Stage II Uterine Corpus Cancer|Stage III Uterine Corpus Cancer|Stage IV Uterine Corpus Cancer Gynecologic Oncology Group|National Cancer Institute (NCI)|GOG Foundation January 2100 --
NCT05118594 Not yet recruiting Behavioral: Pre-treatment psychotherapy recommendations Major Depressive Disorder|Dysthymic Disorder|Specific Phobia|Social Anxiety Disorder|Panic Disorder|Agoraphobia|Generalized Anxiety Disorder National Council of Scientific and Technical Research Argentina February 2026 Not Applicable
NCT03070132 Not yet recruiting Drug: BIIB074|Drug: Placebo Trigeminal Neuralgia Biogen April 19 2023 Phase 3
NCT05182437 Not yet recruiting Radiation: LINAC-based Stereotactic Radiotherapy Epilepsy Maastricht Radiation Oncology|Maastricht University Medical Center|UMC Utrecht|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|ZonMw: The Netherlands Organisation for Health Research and Development January 1 2023 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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