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Doxifluridine

Catalog No. T1600 CAS 3094-09-5

Synonyms: Ro 21-9738, AMC 0101, 5'-DFUR, 5-Fluoro-5'-deoxyuridine

Doxifluridine (AMC 0101) is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.

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Doxifluridine, CAS 3094-09-5

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500 mg	In stock	$ 45.00
1 g	In stock	$ 67.00

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Purity: 99.96%

Purity: 99.86%

Purity: 99.81%

Purity: 99.57%

Biological Description

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Description	Doxifluridine (AMC 0101) is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.
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]

Synonyms	Ro 21-9738, AMC 0101, 5'-DFUR, 5-Fluoro-5'-deoxyuridine
Molecular Weight	246.19
Formula	C9H11FN2O5
CAS No.	3094-09-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 45 mg/mL (182.8 mM)

DMSO: 46 mg/mL (186.8 mM)

References and Literature

1. Naganuma Y, et al. Cancer Sci,2011, 102(8), 1545-1552. 2. Berne M, et al. Cancer Invest,1988, 6(4), 377-383. 3. Baek IH, et al. Eur J Drug Metab Pharmacokinet,2013, 38(4), 295-299. 4. Yamamoto S, et al. Gan To Kagaku Ryoho,1999, 26(10), 1443-1448. 5. Konishi H, et al. J Pharm Pharmacol,2003, 55(1), 143-149.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max Drug-Fragment Library Target-Focused Phenotypic Screening Library Chemotherapy Drug Library Reprogramming Compound Library

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Keywords

Doxifluridine 3094-09-5 Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Ro 21-9738 Inhibitor AMC 0101 5'-DFUR AMC-0101 5-Fluoro-5'-deoxyuridine AMC0101 inhibit inhibitor

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