Fluorouracil (5-Fluoracil, 5-FU)

製品コードS1209 別名:NSC 19893

Fluorouracil (5-Fluoracil, 5-FU)化学構造


Fluorouracil (5-Fluoracil, 5-FU)は一種のDNA/RNA合成阻害剤ですが、腫瘍細胞の中にチミジル酸合成酵素(thymidylate synthase)を抑制することで、ヌクレオチド(nucleotide)の合成を妨害します。

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  • 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.


DNA/RNA Synthesis阻害剤の選択性比較


製品説明 Fluorouracil (5-Fluoracil, 5-FU)は一種のDNA/RNA合成阻害剤ですが、腫瘍細胞の中にチミジル酸合成酵素(thymidylate synthase)を抑制することで、ヌクレオチド(nucleotide)の合成を妨害します。
Thymidylate synthase [1]
(Tumor cells)

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 M{H6WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm3eldMPzMEoHlCpC=> MnGzTWM2OD1{MDFOwIcwdUx? MlruNlQxQTVzN{[=
HT-29 M2jSeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULtSZo6PzMEoHlCpC=> MXrJR|UxRiB{NTFOwIcwdUx? NHrHVJgzPDB7NUG3Oi=>
HL-60 NUHncHVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1SwfFczyqCqwrC= M3LJcGlEPTB;OD62NFEh|rypL33M Mn3nNlQxQTVzN{[=
NCI-H292 NYPSeJlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jmSVczyqCqwrC= NYfEflg3UUN3ME6gNlUh|rypL33M NHrtSmYzPDB7NUG3Oi=>


体内試験 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]


細胞試験: [4]
+ 展開
  • 細胞株: Human colon carcinoma cell line HT-29
  • 濃度: ~25 μM
  • 反応時間: 7 days
  • 実験の流れ: 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.
+ 展開
  • 動物モデル: Murine colon carcinomas Colon 38
  • 製剤: PBS
  • 投薬量: 100 mg/kg
  • 投与方法: i.p. weekly

溶解度 (25°C)

体外 DMSO 26 mg/mL (199.87 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
saline (warming)

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 130.08


CAS No. 51-21-8
別名 NSC 19893





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01928290 Recruiting Stomach Neoplasms|Esophageal Neoplasms Washington University School of Medicine November 8, 2013 Phase 2
NCT00193882 Completed Esophagus Cancer Trans-Tasman Radiation Oncology Group (TROG)|National Health and Medical Research Council, Australia|Canadian Cancer Trials Group July 7, 2003 Phase 3
NCT03050814 Not yet recruiting Colorectal Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 3, 2017 Phase 2
NCT02997228 Not yet recruiting Colorectal Adenocarcinoma|High-Frequency Microsatellite Instability|Stage IV Colorectal Cancer|Stage IVA Colorectal Cancer|Stage IVB Colorectal Cancer National Cancer Institute (NCI) November 2017 Phase 3
NCT02912559 Not yet recruiting Colon Adenocarcinoma|DNA Repair Disorder|Lynch Syndrome|Microsatellite Instability|Stage IIIA Colon Cancer|Stage IIIB Colon Cancer|Stage IIIC Colon Cancer National Cancer Institute (NCI) September 2017 Phase 3
NCT03043547 Not yet recruiting Cholangiocarcinoma Non-resectable|Cholangiocarcinoma Metastatic|Cholangiocarcinoma of the Gallbladder|Cholangiocarcinoma Advanced AIO-Studien-gGmbH|Baxalta GmbH|Shire May 2017 Phase 2



Handling Instructions


  • * 必須


  • 問題1:

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

  • 回答:

    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信号経路図

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID