Fluorouracil (5-Fluoracil, 5-FU)

製品コードS1209 別名:NSC 19893

Fluorouracil (5-Fluoracil, 5-FU)化学構造

分子量(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.

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In DMSO JPY 24200 あり
JPY 26400 あり
JPY 38500 あり
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文献中Selleckの製品使用例(52)

製品安全説明書

DNA/RNA Synthesis阻害剤の選択性比較

生物活性

製品説明 Fluorouracil (5-Fluoracil, 5-FU) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells.
ターゲット
Thymidylate synthase [1]
(Tumor cells)
体外試験

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.

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 NY\iZ5h4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHEdnBnPzMEoHlCpC=> MkjVTWM2OD1{MDFOwIcwdUx? MoG3NlQxQTVzN{[=
HT-29 M3mwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXK3NuKhcMLi Mor4TWM2OD5iMkWg{txoN22O Mm\iNlQxQTVzN{[=
HL-60 NIfWVmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm3NuKhcMLi NH3obolKSzVyPUiuOlAyKM7:Zz;tUC=> NUDmNHpOOjRyOUWxO|Y>
NCI-H292 NYHETWNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[2O|LDqGkEoB?= M2[yXmlEPTB-IEK1JO69\y:vTB?= MkPGNlQxQTVzN{[=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
p53 / PUMA / c-PARP; 

PubMed: 25965911     


(A) HCT-116 cells were treated with various doses of 5-FU for 24 hours (B) HCT-116 cells were treated with 200 uM 5-FU, then harvested at different time points after stimulation. The expression of p53, PUMA, cleaved PARP and P-Akt(S473) were detected by western blotting in different conditions.

25965911
Immunofluorescence
caveolin-3; 

PubMed: 23646193     


Cells were stained with an antibody against caveolin-3 (green) and with DAPI (blue). (A) control cells (top images), 10 mM 5-FU (middle images), 50 mM 5-FU (bottom images). Merged images are shown at the right of each panel.

phospho-histone H3 ; 

PubMed: 23646193     


Cells were grown for 24 h, treated with 5-FU and stained with an anti-phospho-histone H3 antibody (red) and with DAPI (blue). (A) control cells, (B) 0.1 mM 5-FU and (C) 1 mM 5-FU. 

p65 / p-p65(Ser536) / p53 / p-p53(Ser15); 

PubMed: 24587255     


E–H, Immunocytochemistry of p65 and p53 induction and localization by 5-FU treatment for the indicated cell lines. p65 (red), phosphor-p65 (Ser536; red), p53 (green), phospho-p53 (Ser15; red), and DAPI (blue) staining of the nucleus without (control) and with 5-FU treatment. 

Sox2 / Oct4 / Nanog / ABCG2; 

PubMed: 27009861     


(A) Immunofluorescence staining of Sox2, Oct4 and Nanog in HBE cells with or without 5-FU treatment. In untreated HBE cells, few Sox2, Oct4 or Nanog-positive cells were observed. After 5-FU treatment, the number of Sox2, Oct4 or Nanog-positive cells increased remarkably. Nuclei were counterstained with DAPI (blue). (B) Immunofluorescence staining of ABCG2 in HBE cells with or without 5-FU treatment. 

β-catenin; 

PubMed: 30111797     


Immunofluorescence detection of β-catenin in HCT-8 cells. Scale bar, 20 μm.

non-phospho β-catenin; 

PubMed: 28588704     


Effect of enhanced WNT signaling in Ell3 OE cells. Localization of non-phosphorylated β-catenin was analyzed by immunocytochemical staining in (A) control MCF-7 and (B) Ell3 OE treated with various 5-FU concentrations.

23646193 24587255 27009861 30111797 28588704
Growth inhibition assay
Cell viability; 

PubMed: 25965911     


Cells viability was analyzed using Cell Counting Kit-8 at 0, 3, 6, 12 and 24 hours after (A) 50, 100, 200, or 400 uM 5-FU treatment in HCT116 cells.

Cell proliferation; 

PubMed: 30250641     


(A) Cell proliferation assay with resveratrol in HCT116. Cells were treated with resveratrol at 0 ~ 200 μM for 72 hours and applied to MTS assay. (B) HCT116 cells were treated with 5-FU at 0~200 μM for 72 hours. (C)HCT116 cells were treated with resveratrol at 0 ~ 200 μM combined with 5-FU at 10 μM for 72 hours and applied to MTS assay. (D) DLD1 cell proliferation assay with resveratrol at 0 ~ 200 μM for 72 hours. (E) DLD1 cells were treated with 5-FU at 0~ 200 μM for 72 hours. (F) DLD1 cells were treated with resveratrol combined with 5-FU at 10 μM for 72 hours. Error bars represent standard deviation.

25965911 30250641
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]

お薦めの試験操作(参考用のみ)

細胞試験: [4]
- 合併
  • 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.
    (参考用のみ)
動物試験:[5]
- 合併
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 26 mg/mL (199.87 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
saline (warming)
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 130.08
化学式

C4H3FN2O2

CAS No. 51-21-8
保管
in solvent
別名 NSC 19893

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

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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