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Doxifluridine Phosphorylase activator

Name: Doxifluridine
Brand: Selleck Chemicals
SKU: S2045
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S2045

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

Chemical Structure

Molecular Weight: 246.19

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.76%

99.76

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite Casein Kinase Serine/threonin kinase Lipoxygenase LPL Receptor Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase Glucokinase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO
Related Products	CP-91149 Ingliforib Iso-H7 dihydrochloride Thymidine Phosphorylase Antibody [E2G2]

Chemical Information, Storage & Stability

Molecular Weight	246.19	Formula	C₉H₁₁FN₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	3094-09-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	5'-DFUR, AMC 0101			Smiles	CC1C(C(C(O1)N2C=C(C(=O)NC2=O)F)O)O

Solubility

In vitro
Batch:

DMSO : 49 mg/mL (199.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 49 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

In vitro	Doxifluridine suppresses tube formation of HUVEC and vascular endothelial growth factor production by FU-MMT-1 cells. ^[1] This compound is converted to 5-FU and subsequently to FdUMP, and the results suggest that it exerts its cytotoxic effects through inhibition of TS and incorporation into RNA. ^[2] It is a fluoropyrimidine derivative that is activated preferentially in malignant cells by thymidine phosphorylase to form 5-fluorouracil (5-FU). This chemical 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 this compound in combination with TNP-470 significantly inhibits tumor growth compared with each treatment alone in in FU-MMT-1 xenografts. This compound in combination with TNP-470 also leads to a significant reduction of intratumoral vascularity. ^[1] It 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] This chemical results in a significant reduction in the activity of phenytoin p-hydroxylation in rats. It decreases the elimination rate constant and the total clearance in rats. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/21631643/ [2] https://pubmed.ncbi.nlm.nih.gov/2972339/ [3] https://pubmed.ncbi.nlm.nih.gov/23564503/ [4] https://pubmed.ncbi.nlm.nih.gov/10500532/ [5] https://pubmed.ncbi.nlm.nih.gov/12625878/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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