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5-Fluorouracil

カタログ番号 T0984   CAS 51-21-8
別名: 5-FU, Fluorouracil, NSC 19893, 5-Fluoracil

5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy.

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5-Fluorouracil, CAS 51-21-8
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100 mg 在庫あり ¥ 7,000
1 g 在庫あり ¥ 11,000
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生物学的特性に関する説明
化学的特性
保存条件 & 溶解度情報
説明 5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy.
In vitro METHODS: Human cardiomyocytes HCM, human umbilical vein endothelial cells HUVE, and human colon cancer cells HCT116 and HT29 were treated with 5-Fluorouracil (0.01-1000 µM) for 24-96 h, and the growth inhibition of the cells was detected by MTT.
RESULTS: The EC50 of 5-Fluorouracil on HCM, HUVE, PHCT116 and HT29 cells were 4.866 μM, 3.832 μM, 13.72 μM and 106.8 μM, respectively, at 72 h. [1]
METHODS: Smooth muscle cells were treated with 5-Fluorouracil (0.05-10 mM) for 24 h. Apoptosis was detected using Flow Cytometry.
RESULTS: 5-Fluorouracil at concentrations of 0.1, 1, and 10 mM induced apoptosis in cultured smooth muscle cells after 24 h of treatment, and the apoptotic cells were detached from the culture dishes. [2]
METHODS: Human colon cancer cells SW620 were incubated with 5-Fluorouracil (13 μg/mL) for 24-48 h. ALP activity was detected using an ALP detection kit.
RESULTS: Alkaline phosphatase (ALP) has been used to monitor the differentiation effects of certain anticancer compounds. Untreated SW620 cells showed relatively low ALP activity, while in cells treated with 13 μg/ml 5-FU, ALP activity reached high levels in a time-dependent manner. [3]
In vivo METHODS: To detect the antitumor activity in vivo, 5-Fluorouracil (10-40 mg/kg) was injected intraperitoneally once a day for ten days into mice bearing ascites hepatocellular carcinoma tumor H22.
RESULTS: 5-Fluorouracil at 10 mg/kg inhibited tumor growth while maintaining immune function in mice. 5-Fluorouracil exerts low-dose, low-toxicity antitumor effects and stimulates the host immune system. [4]
METHODS: To study 5-Fluorouracil-induced intestinal injury, 5-Fluorouracil (100-200 mg/kg) was administered as a single intraperitoneal injection to BALB/c mice.
RESULTS: The body weight and diarrhea symptoms of 5-Fluorouracil-treated animals were significantly reduced in a dose-dependent manner. Occludin and claudin-1 protein expression was significantly reduced in the 5-Fluorouracil-treated group. 5-Fluorouracil-treated group showed significantly higher NF-κBp65 protein and TNF-α mRNA expression than the control group. NF-κBp65 protein and TNF-α mRNA expression were significantly higher in the 5-Fluorouracil treated group than in the control group. [5]
細胞研究 After a 7-day habituation period, the mice were divided into three groups (vehicle group, dextrin group, and ED group; n = 6 mice per group) that had the same mean body weight (time of grouping was designated as day 0). Then, mice were treated by tail vein injections from day 0 to 4; mice in the dextrin and ED groups received 40 mg/kg/day of 5- fluorouracil (5-FU) injection 250 mg, while mice in the vehicle group received 10 mL/kg/day physiological saline, which was equivalent to the dose of 5-FU. Additionally, twice a day from day 0 to 6, ED group mice received 1.6 kcal/0.8 mL/day ED administered orally, while mice in the vehicle and dextrin groups received dextrin containing the same amount of calories. Body weight and food consumption were measured before administration of 5-FU and ED on days 0 and 7. Food consumption was measured with respect to each group. Mice were accommodated individually in specially prepared polycarbonate cages, and two or more fresh stools per mouse were scored as follows: 0, the stools were not crushed when pushed by human fingers; 1, the stools were crushed, but the core remained when pushed by human fingers; 2, the stools were crushed and the core did not remain when pushed by human fingers; 3, the stools were crushed and stuck to the fingers when pushed by human fingers; 4, the stools lost their shape just from being touched. Autopsies were conducted on day 7. After bleeding, the large intestine (the colon and rectum) was taken, and the length was measured. The lumen was washed with physiological saline, the excess water was wiped off, and specimens were weighed. Section 3 cm distal from the center of the large intestine was fixed with formalin for histological evaluation. Salivary glands (the submandibular gland and sublingual gland) were collected and weighed. The collected salivary glands were fixed with formalin, and after the tissue sections were prepared, they were stained with hematoxylin and eosin [3].
別名 5-FU, Fluorouracil, NSC 19893, 5-Fluoracil
分子量 130.08
分子式 C4H3FN2O2
CAS No. 51-21-8

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

Ethanol: 1.3 mg/mL (10 mM)

DMSO: 18.33 mg/mL (140.94 mM)

参考文献

1. Focaccetti C, et al. Effects of 5-fluorouracil on morphology, cell cycle, proliferation, apoptosis, autophagy and ROS production in endothelial cells and cardiomyocytes. PLoS One. 2. Filgueiras Mde C, et al. Effects of 5-fluorouracil in nuclear and cellular morphology, proliferation, cell cycle, apoptosis, cytoskeletal and caveolar distribution in primary cultures of smooth muscle cells. PLoS One. 2013 Apr 30;8(4):e63177. 3. Gao L, et al. Colon cancer cells treated with 5‑fluorouracil exhibit changes in polylactosamine‑type N‑glycans. Mol Med Rep. 2014 May;9(5):1697-702. 4. Cao Z, et al. Antitumor and immunomodulatory effects of low-dose 5-FU on hepatoma 22 tumor-bearing mice. Oncol Lett. 2014 Apr;7(4):1260-1264. 5. Song MK, et al. 5-Fluorouracil-induced changes of intestinal integrity biomarkers in BALB/c mice. J Cancer Prev. 2013 Dec;18(4):322-9. 6. Yin L, et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer in vitro and in vivo. Ther Clin Risk Manag. 2017 Feb 7;13:117-130. 7. Kim W, Park C, Park J, et al. Pine needle hexane extract promote cell cycle arrest and premature senescence via p27 KIP1 upregulation gastric cancer cells[J]. Food Science and Biotechnology. 2020: 1-9. 8. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma[J]. Cancer Research.

引用文献

1. Zhao X, Lian X, Xie J, et al.Accumulated cholesterol protects tumours from elevated lipid peroxidation in the microenvironment.Redox Biology.2023: 102678. 2. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 3. Zhang S, Sun Y, Yao F, et al.Ginkgo Biflavones Cause p53 Wild-Type Dependent Cell Death in a Transcription-Independent Manner of p53.Journal of Natural Products.2023 4. Ouyang S, Li H, Lou L, et al. Inhibition of STAT3-ferroptosis negative regulatory axis suppresses tumor growth and alleviates chemoresistance in gastric cancer. Redox Biology. 2022: 102317 5. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 6. Li Q, Lai Q, He C, et al. RUNX1 regulates the proliferation and chemoresistance of colorectal cancer through the Hedgehog signaling pathway. Journal of Cancer. 2021, 12(21): 6363-6371. 7. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021 Mar 1;81(5):1413-1425. doi: 10.1158/0008-5472.CAN-20-2125. Epub 2021 Jan 5. 8. Xu X, Zhang S, Wang Y, et al. Virtual Screening Inhibitors of Ubiquitin-specific Protease 7 combining Pharmacophore Modeling and Molecular Docking. Molecular Informatics. 2022 9. Liu L, Liu S, Deng P, et al. Targeting the IRAK1–S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021, 81(5): 1413-1425. 10. Luo X, Cai G, Guo Y, et al. Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer. Journal of Medicinal Chemistry..
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関連化合物ライブラリー

この製品は下記化合物ライブラリに含まれています:
Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Apoptosis Compound Library Bioactive Compounds Library Max DNA Damage & Repair Compound Library ReFRAME Related Library

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投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください
投与量
mg/kg
動物の平均体重
g
動物あたりの投与量
ul
動物数
溶媒の組成を入力してください
% DMSO
%
% Tween 80
% ddH2O
計算する リセット

計算器

モル濃度計算機
希釈計算機
再構成計算
分子量計算機
=
X
X

モル度計算機では以下の計算が可能です

  • 既知の体積と濃度の溶液を調製するために必要な化合物の質量
  • 質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
  • 特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度
参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか?
[分子量(MW)]の欄に[197.13]と入力してください
[濃度]ボックスに10と入力し、正しい単位(millimolar)を選択します
[容量]ボックスに10と入力し、正しい単位(milliliter)を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

X
=
X

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2&V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか?
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度(開始)ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度(終了)ボックスに50を入力し正しい単位(millimolar)を選択してください
体積(終了)ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積(開始)ボックスに表示されます。

=
/

バイアルを再構成するのに必要な溶媒の量を計算する.

再構成計算機を使えば、バイアルを再構成するための試薬の量をすぐに計算することができます.
試薬の質量と目標濃度を入力するだけで計算します。

g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント:化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量(分子量)を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量(分子量)とは、物質の1分子の質量であり、統一された原子質量単位(u)で表されます。(1uは炭素12の1原子の質量の1/12に等しい)
モル質量(molar weight)とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

5-Fluorouracil 51-21-8 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Microbiology/Virology Proteases/Proteasome Nucleoside Antimetabolite/Analog HIV Protease Endogenous Metabolite DNA/RNA Synthesis 5-FU 5 Fluorouracil inhibit Fluorouracil NSC19893 Inhibitor 5Fluorouracil Human immunodeficiency virus HIV NSC 19893 5-Fluoracil NSC-19893 inhibitor