5-Fluorouracil (5-FU)

製品コードS1209 バッチS120906

印刷

化学情報

Chemical Structure Synonyms Fluorouracil, NSC 19893 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C4H3FN2O2
分子量 130.08 CAS No. 51-21-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (768.75 mM)
Water 8 mg/mL (61.5 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
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.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.650mg/ml (5.00mM) Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 3.500mg/ml (26.91mM) Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 5-FU (5-Fluorouracil) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.
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.
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]

プロトコル(参考用のみ)

細胞アッセイ 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.
動物実験 動物モデル Murine colon carcinomas Colon 38
投薬量 100 mg/kg
投与方法 i.p. weekly

参考

  • https://pubmed.ncbi.nlm.nih.gov/12724731/
  • https://pubmed.ncbi.nlm.nih.gov/18452707/
  • https://pubmed.ncbi.nlm.nih.gov/12138244/
  • https://pubmed.ncbi.nlm.nih.gov/7642571/
  • https://pubmed.ncbi.nlm.nih.gov/8995503/

カスタマーフィードバック

Data from [Data independently produced by Mol Cell Biochem, 2014, 10.1007/s11010-014-2253-6]

Data from [Data independently produced by , , J Invest Dermatol, 2018, 138(8):1716-1725]

Data from [Data independently produced by , , Eur Rev Med Pharmacol Sci, 2016, 20(9):1699-706.]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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