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Doxifluridine

Doxifluridine

产品编号 T1600   CAS 3094-09-5
别名: Ro 21-9738, AMC 0101, 5'-DFUR, 5-Fluoro-5'-deoxyuridine, 去氧氟尿苷

Doxifluridine (AMC 0101) 是一种胸苷磷酸化酶活化剂,对 PC9-DPE2细胞的 IC50为0.62 μM。它是具有抗肿瘤活性的抗肿瘤剂 5-fluorouracil (5-FU) 的氟嘧啶衍生物和口服前药。

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Doxifluridine Chemical Structure
Doxifluridine, CAS 3094-09-5
规格 价格/CNY 货期 数量
500 mg ¥ 414 现货
1 g ¥ 498 现货
产品目录号及名称: Doxifluridine (T1600)
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纯度: 99.96%
纯度: 99.86%
纯度: 99.81%
纯度: 99.57%
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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 Doxifluridine (AMC 0101) is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.
体外活性 Doxifluridine suppresses tube formation of HUVEC and vascular endothelial growth factor production by FU-MMT-1 cells. [1] Doxifluridine is converted to 5-FU and subsequently to FdUMP, and the results suggest that Doxifluridine exerts its cytotoxic effects through inhibition of TS and incorporation into RNA. [2] Doxifluridine is a fluoropyrimidine derivative that is activated preferentially in malignant cells by thymidine phosphorylase to form 5-fluorouracil (5-FU). Doxifluridine is developed to improve the therapeutic index of 5-FU and to reduce toxicity, including the immunosuppressive, myelosuppressive, and cardiotoxic effects of 5-FU and other fluorinated pyrimidines. [3]
体内活性 Metronomic Doxifluridine alone significantly suppresses tumor growth compared with the untreated (control) group, while metronomic Doxifluridine in combination with TNP-470 significantly inhibits tumor growth compared with each treatment alone in in FU-MMT-1 xenografts. Doxifluridine in combination with TNP-470 also leads to a significant reduction of intratumoral vascularity. [1] Doxifluridine significantly inhibits the growth of KPL-4 tumors, reduces the tissue levels of IL-6, and alleviates body weight loss in nude mice bearing KPL-4 tumors. [4] Doxifluridine results in a significant reduction in the activity of phenytoin p-hydroxylation in rats. Doxifluridine decreases the elimination rate constant and the total clearance in rats. [5]
别名 Ro 21-9738, AMC 0101, 5'-DFUR, 5-Fluoro-5'-deoxyuridine, 去氧氟尿苷
分子量 246.19
分子式 C9H11FN2O5
CAS No. 3094-09-5

存储

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

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 45 mg/mL (182.8 mM)

DMSO: 46 mg/mL (186.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.0619 mL 20.3095 mL 40.619 mL 101.5476 mL
5 mM 0.8124 mL 4.0619 mL 8.1238 mL 20.3095 mL
10 mM 0.4062 mL 2.031 mL 4.0619 mL 10.1548 mL
20 mM 0.2031 mL 1.0155 mL 2.031 mL 5.0774 mL
50 mM 0.0812 mL 0.4062 mL 0.8124 mL 2.031 mL
100 mM 0.0406 mL 0.2031 mL 0.4062 mL 1.0155 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Naganuma Y, et al. Cancer Sci,2011, 102(8), 1545-1552. 2. Berne M, et al. Cancer Invest,1988, 6(4), 377-383. 3. Baek IH, et al. Eur J Drug Metab Pharmacokinet,2013, 38(4), 295-299. 4. Yamamoto S, et al. Gan To Kagaku Ryoho,1999, 26(10), 1443-1448. 5. Konishi H, et al. J Pharm Pharmacol,2003, 55(1), 143-149.
Daunorubicin hydrochloride UNC9512 Antiviral agent 36 DNA Gyrase-IN-8 S-Adenosyl-L-methionine disulfate tosylate DNA gyrase B-IN-3 Deoxycytidine triphosphate trisodium salt Ribavirin

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌上市药物库 抗癌临床化合物库 药物代谢杂质库 肝脏毒性化合物库 已知活性化合物库 细胞周期化合物库 免疫/炎症分子化合物库 抗癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
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。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

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

Doxifluridine 3094-09-5 Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Ro 21-9738 Inhibitor AMC 0101 5'-DFUR AMC-0101 5-Fluoro-5'-deoxyuridine AMC0101 去氧氟尿苷 inhibit inhibitor

 

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