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5-Fluorouracil

5-Fluorouracil

产品编号 T0984   CAS 51-21-8
别名: 5-FU, Fluorouracil, 5-氟脲嘧啶, NSC 19893, 5-Fluoracil, 氟尿嘧啶

5-Fluorouracil (5-FU) 是一种尿嘧啶类似物,一种 DNA 合成抑制剂。5-Fluorouracil 具有抗肿瘤活性,通过抑制胸苷酸合成酶影响嘧啶的合成。5-Fluorouracil 可以引起细胞凋亡自噬

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5-Fluorouracil Chemical Structure
5-Fluorouracil, CAS 51-21-8
规格 价格/CNY 货期 数量
200 mg ¥ 291 现货
1 g ¥ 375 现货
5 g ¥ 696 现货
1 mL * 10 mM (in DMSO) ¥ 418 现货
其他形式的 5-Fluorouracil:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: 5-Fluorouracil (T0984)
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纯度: 100%
纯度: 100%
纯度: 99.83%
纯度: 99.56%
纯度: 99.56%
纯度: 98.77%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
体外活性 方法:人心肌细胞 HCM、人脐静脉内皮细胞 HUVE 和 人结肠癌细胞 HCT116、HT29 用 5-Fluorouracil (0.01-1000 µM) 处理 24-96 h,使用 MTT 方法检测细胞生长抑制情况。
结果:72 h 时 5-Fluorouracil 对 HCM、HUVE、PHCT116 和 HT29 细胞的 EC50 分别为 4.866 μM、3.832 μM、13.72 μM 和 106.8 μM。[1]
方法:平滑肌细胞用 5-Fluorouracil (0.05-10 mM) 处理 24 h,使用 Flow Cytometry 方法检测细胞凋亡情况。
结果:浓度为 0.1、1 和 10mM 的 5-Fluorouracil 在处理 24 h 后诱导培养的平滑肌细胞凋亡,并且凋亡细胞从培养皿中分离。[2]
方法:人结肠癌细胞 SW620 用 5-Fluorouracil (13 μg/mL) 孵育 24-48 h,使用 ALP detection kit 检测 ALP 活性。
结果:碱性磷酸酶 (ALP) 已被用于监测某些抗癌化合物的分化效果。未处理的 SW620 细胞表现出相对较低的 ALP 活性,而在用 13μg/ml 5-FU 处理的细胞中,ALP 的活性以时间依赖的方式达到高水平。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 5-Fluorouracil (10-40 mg/kg) 腹腔注射给携带小鼠腹水肝癌肿瘤 H22 的小鼠,每天一次,持续十天。
结果:10 mg/kg 的 5-Fluorouracil 抑制肿瘤生长,同时维持小鼠的免疫功能。5-Fluorouracil 可发挥低剂量、低毒的抗肿瘤作用,刺激宿主免疫系统。[4]
方法:为研究 5-Fluorouracil 诱导的肠道损伤,将 5-Fluorouracil (100-200 mg/kg) 单次腹腔注射给 BALB/c 小鼠。
结果:5-Fluorouracil 治疗的动物的体重及腹泻症状以剂量依赖的方式显著降低。5-Fluorouracil 治疗组的 occludin 和 claudin-1 蛋白的表达显著降低。5-Fluorouracil 治疗组 NF-κBp65 蛋白和 TNF-α mRNA 的表达明显高于对照组。[5]
细胞实验 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].
别名 5-FU, Fluorouracil, 5-氟脲嘧啶, NSC 19893, 5-Fluoracil, 氟尿嘧啶
分子量 130.08
分子式 C4H3FN2O2
CAS No. 51-21-8

存储

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

溶解度

Ethanol: 1.3 mg/mL (10 mM)

DMSO: 13 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 7.6876 mL 38.4379 mL 76.8758 mL 192.1894 mL
5 mM 1.5375 mL 7.6876 mL 15.3752 mL 38.4379 mL
10 mM 0.7688 mL 3.8438 mL 7.6876 mL 19.2189 mL
DMSO 20 mM 0.3844 mL 1.9219 mL 3.8438 mL 9.6095 mL
50 mM 0.1538 mL 0.7688 mL 1.5375 mL 3.8438 mL
100 mM 0.0769 mL 0.3844 mL 0.7688 mL 1.9219 mL

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TargetMol Library Books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.

TargetMol Library Books文献引用

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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相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗癌药物库 抗癌临床化合物库 抑制剂库 抗癌活性化合物库 药物功能重定位化合物库 抗COVID-19化合物库 毒性化合物库 化疗药物库 细胞重编程化合物库

TargetMol Calculator剂量换算

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

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 5-氟脲嘧啶 Human immunodeficiency virus HIV NSC 19893 5-Fluoracil NSC-19893 氟尿嘧啶 inhibitor

 

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