Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 45 mg/mL (182.8 mM)
DMSO: 46 mg/mL (186.8 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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