Fluorouracil (5-Fluoracil, 5-FU)

Catalog No.S1209 Synonyms: NSC 19893

Fluorouracil (5-Fluoracil, 5-FU) Chemical Structure

Molecular Weight(MW): 130.08

Fluorouracil (5-Fluoracil, 5-FU) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells.

Size Price Stock Quantity  
In DMSO USD 134 In stock
USD 147 In stock
USD 220 In stock
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2 Customer Reviews

  • DNA-PKcs suppression mediated ROS production and GSH content in HepG2 cells exposed to CDDP and 5-Fu. a DNA-PKcs inhibition promoted ROS production in HepG2 cells treated with indicated concentrations of CDDP and 5-Fu. DCFH-DA fluorescent analysis was performed to assess the ROS level. Data presented were mean ?SD of three independent experiments.

    Mol Cell Biochem 2014 10.1007/s11010-014-2253-6. Fluorouracil (5-Fluoracil, 5-FU) purchased from Selleck.

    EdU staining of RBE cells treated with OSI-027 (6.25 μM) and/or 5-FU (6.25 μg/mL) was performed by using Click-iT EdU Imaging Kit. The percentages of EdU-positive cells have been provided in the right panel.

    Eur Rev Med Pharmacol Sci, 2016, 20(9):1699-706.. Fluorouracil (5-Fluoracil, 5-FU) purchased from Selleck.

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Biological Activity

Description Fluorouracil (5-Fluoracil, 5-FU) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells.
Targets
Thymidylate synthase [1]
(Tumor cells)
In vitro

Adrucil is an analogue of uracil with a fluorine atom at the C-5 position in place of hydrogen. It rapidly enters the cell using the same facilitated transport mechanism as uracil. Adrucil is converted intracellularly to several active metabolites: fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine triphosphate (FUTP). The Adrucil metabolite FdUMP binds to the nucleotide-binding site of TS, forming a stable ternary complex with the enzyme and CH2THF, thereby blocking binding of the normal substrate dUMP and inhibiting dTMP synthesis. Metabolite of Adrucil also can be misincorporated into DNA, leading to DNA strand breaks and cell death. The pro-apoptosis effects of Adrucil may be related to its activation of tumor suppressor p53. Loss of p53 function reduces cellular sensitivity to Adrucil. [1] Adrucil is able to inhibit the survival and induce apoptosis of a board range of cancer cells. Adrucil suppresses viabilities of the nasopharyngeal carcinoma cell line CNE2 and HONE1 [2], pancreatic cancer cell lines Capan-1 [3], and human colon carcinoma cell line HT-29 [4] with IC50 of 9 μg/mL, 3 μg/mL, 0.22 μM, 2.5 μM, respectively.

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 NGLP[Y9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXqTIRtPzMEoHlCpC=> M4LyVGlEPTB;MkCg{txoN22O NV25cpI6OjRyOUWxO|Y>
HT-29 M1S1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXuzeJE4PzMEoHlCpC=> MkPxTWM2OD5iMkWg{txoN22O MVqyOFA6PTF5Nh?=
HL-60 NIjofFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\Jb5Y4OsLiaNMg NFry[JJKSzVyPUiuOlAyKM7:Zz;tUC=> NH7VcpUzPDB7NUG3Oi=>
NCI-H292 NVPkN2V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rab|czyqCqwrC= NVjFPGJGUUN3ME6gNlUh|rypL33M NHjiVo4zPDB7NUG3Oi=>

... Click to View More Cell Line Experimental Data

In vivo Adrucil is widely used in the treatment of a range of cancers, including colorectal and breast cancers. [1] 100mg/kg Adrucil significantly suppresses tumor growth of murine colon carcinomas Colon 38 with tumor-doubling time (TD), growth-delay factor (GDF), and T/C of 26.5 days, 4.4, and 14%. [5]

Protocol

Cell Research:[4]
+ Expand
  • Cell lines: Human colon carcinoma cell line HT-29
  • Concentrations: ~25 μM
  • Incubation Time: 7 days
  • Method: Growth inhibition is measured after treatment of cells with Adrucil for 7 days in 96-well plates (4000 HT-29 cells/well in RPMI 1640 medium with 10% dialyzed fetal bovine serum); increasing concentrations of Adrucil are added after allowing for cell attachment overnight. At the end of incubation, cells are rinsed three times with phosphate-buffered saline (pH 7.4), fixed with 10% trichloroacetic acid for 60 min at 4 ℃, washed five times with deionized water, and stained with 0.4% sulforhoda-mine B solution for 15 min at room temperature. Unstained sulforhodamine B is removed by rinsing with 1% glacial acetic acid. Afterwards, stained cell proteins are dried and dissolved with 10 mM Tris-HCl. The optical density value is measured using a detector at 540 nm wavelength.
    (Only for Reference)
Animal Research:[5]
+ Expand
  • Animal Models: Murine colon carcinomas Colon 38
  • Formulation: PBS
  • Dosages: 100 mg/kg
  • Administration: i.p. weekly
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 26 mg/mL (199.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
saline (warming)
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 130.08
Formula

C4H3FN2O2

CAS No. 51-21-8
Storage powder
in solvent
Synonyms NSC 19893

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03541252 Recruiting Carcinoma Basal Cell Merete Haedersdal|Bispebjerg Hospital July 9 2018 Phase 1|Phase 2
NCT03221426 Recruiting Gastric Cancer|Gastroesophageal Junction Cancer Merck Sharp & Dohme Corp. October 9 2017 Phase 3
NCT01566435 Active not recruiting Head and Neck Neoplasms Washington University School of Medicine August 9 2012 Phase 2
NCT03446872 Recruiting Metastatic Pancreatic Cancer Shire|Shire Pharma Korea Co. Ltd. March 8 2018 --
NCT01928290 Active not recruiting Stomach Neoplasms|Esophageal Neoplasms Washington University School of Medicine November 8 2013 Phase 2
NCT01523431 Completed Metastatic Colorectal Cancer The Affiliated Hospital of the Chinese Academy of Military Medical Sciences March 8 2012 Phase 2|Phase 3

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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.

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Frequently Asked Questions

  • Question 1:

    I was wondering if the product #s1209 (5-fluorouracil) is suitable to inject into mice ?

  • Answer:

    S1209 is suitable to inject (I.P.) into mice as indicating in this paper: http://www.ncbi.nlm.nih.gov/pubmed/8995503.

DNA/RNA Synthesis Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID