5-氟脲嘧啶 T0984

Product Introduction
Bioactivity


英文名: 5-Fluorouracil

描述: 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 可以引起细胞凋亡和自噬。

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].

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]

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

溶解度: Ethanol : 1.3 mg/mL (10 mM)
DMSO : 18.33 mg/mL (140.94 mM)


关键字: 5 Fluorouracil | Endogenous Metabolite | inhibit | Nucleoside Antimetabolite/Analog | NSC19893 | Apoptosis | Inhibitor | 5Fluorouracil | Human immunodeficiency virus | 5-Fluorouracil | HIV | NSC-19893

相关产品: JNJ-7706621 | Nimustine Hydrochloride | Soyasapogenol B | NPS-1034 | Orantinib | TIC10 | ASK1-IN-2 | Nirogacestat | BTdCPU | Apocynin

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Covalent Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途