5-Fluorouracil (5-FU)

製品コードS1209 バッチS120904

印刷

化学情報

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

C4H3FN2O2

分子量 130.08 CAS No. 51-21-8
Solubility (25°C)* 体外 DMSO 26 mg/mL (199.87 mM)
Water 10 mg/mL (76.87 mM)
Ethanol Insoluble
* <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) はDNA/RNA Synthesis阻害剤であり、腫瘍細胞内のThymidylate Synthaseを阻害することでヌクレオチド合成を中断させます。Fluorouracilはapoptosisを誘導し、HIVの治療に用いられます。
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. 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 , pancreatic cancer cell lines Capan-1 , and human colon carcinoma cell line HT-29 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. 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%.

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.]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Homoisoflavanone Delays Colorectal Cancer Progression via DNA Damage-Induced Mitochondrial Apoptosis and Parthanatos-Like Cell Death [ Adv Sci (Weinh), 2026, 13(19):e11406] PubMed: 41603109
RBM15 Enhances 5-Fluorouracil Drug Sensitivity and Suppresses Gastric Cancer Progression by Modulating N6-Methyladenosine Modification of ECT2-Dependent IGF2BP3 [ Research (Wash D C), 2026, 9:1108] PubMed: 41635511
A novel comprehensive mucins relevant subtypes predict chemo-responses in colorectal cancer [ Int J Biol Macromol, 2026, 345:150612] PubMed: 41617007
Target choice and exon skipping regulate CRISPR-directed gene editing of NRF2 in head/neck and esophageal cancer cells [ Mol Ther Oncol, 2026, 34(1):201122] PubMed: 41624405
Dabupi decoction mitigates fluorouracil-induced intestinal mucositis via farnesoid X receptor activation and dihydropyrimidine dehydrogenase upregulation [ J Ethnopharmacol, 2026, 367:121742] PubMed: 42069161
Vitrification-based tissue-to-organoid cryopreservation workflow for colorectal cancer [ N Biotechnol, 2026, 93:341-350] PubMed: 42055114
Roles of GPX4 and FSP1 in Esophageal Squamous Cell Carcinoma Treated With Neoadjuvant Chemotherapy [ Anticancer Res, 2026, 46(3):1529-1543] PubMed: 41760249
Activation of lysosomal iron triggers ferroptosis in cancer [ Nature, 2025, 10.1038/s41586-025-08974-4] PubMed: 40335696
Cisplatin and temozolomide combinatorial treatment triggers hypermutability and immune surveillance in experimental cancer models [ Cancer Cell, 2025, S1535-6108(25)00223-5] PubMed: 40513578
A pancreatic cancer organoid biobank links multi-omics signatures to therapeutic response and clinical evaluation of statin combination therapy [ Cell Stem Cell, 2025, S1934-5909(25)00265-6] PubMed: 40812300

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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