Doxifluridine
产品说明书
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同义名 : | 5'-脱氧-5-氟尿苷 ;5'-DFUR;5-Fluoro-5'-deoxyuridine;5'-Deoxy-5-fluorouridine.;doxyfluridine;Flutron;Furtulon;5-DFUR;AMC 0101;Ro 21-9738 |
| CAS号 : | 3094-09-5 | |
| 货号 : | A137458 | |
| 分子式 : | C9H11FN2O5 | |
| 纯度 : | 98% | |
| 分子量 : | 246.192 | |
| MDL号 : | MFCD00866530 | |
| 存储条件： |
Pure form Inert atmosphere,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(426.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 20 mg/mL(81.24 mM)，配合低频超声助溶 DMF: 100 mg/mL(406.19 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | In tumors, doxifluridine is converted to 5-FU by thymidine phosphorylase (TP). TP, also known asplatelet-derived endothelial cell growth factor, is upregulated in many solid tumors including breast, prostate and colorectal cancers. Elevated levels of TP are associated with tumor aggressionand poor prognosis. Doxifluridine, a derivative of 5-fluorouracil (5-FU) with less severe systemic toxicity, is a TP activator and widely used to treat various cancers. Doxifluridine significantly inhibited tube formation compared with the untreated control group (P< 0.0001). Doxifluridine at 10 μM significantly suppressed VEGF (vascular endothelial growth factor) expression in FU-MMT-1 cells compared with the control group in vitro (P< 0.01). Low-dose doxifluridine (1 μM) slightly increased TSP-1 expression (P = 0.272) in HUVEC, whereas high-dose doxifluridine (100 μM) reduced TSP-1 expression. Low-dose doxifluridine (1 and 10 μM) significantly increased TSP-1 expression in FU-MMT-1 cells compared with the control group (1 μM, P = 0.041; 10 μM, P = 0.0089). Further, doxifluridine (100 μM) reduced the proliferation of HUVEC compared with the control group. Administration of doxifluridine in combination with TNP-470 showed significantly greater suppression of tumor growth compared with either treatment alone. Following treatment, the tumor completely disappeared in five of six (83.3%) mice treated with the MTD (maximum tolerated dose) of doxifluridine in combination with TNP-470[1]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02494596 | - | Completed | - | - | |
| NCT00842244 | Stomach Neoplasms ... 展开 >> Advanced Gastric Cancer 收起 << | Phase 1 | Completed | - | Japan ... 展开 >> Pfizer Investigational Site Kashiwa, Chiba, Japan Pfizer Investigational Site Yufu-city, Oita, Japan Korea, Republic of Pfizer Investigational Site Goyang-si, Gyeonggi-do, Korea, Republic of, 410-769 Pfizer Investigational Site Seongnam-si, Gyeonggi-do, Korea, Republic of, 463-707 Pfizer Investigational Site Seoul, Korea, Republic of, 110-744 收起 << |
| NCT00925769 | Pancreatic Cancer | Phase 1 | Completed | - | Austria ... 展开 >> Vienna, Austria, 1100 Wien, Austria, 1130 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.06mL 0.81mL 0.41mL |
20.31mL 4.06mL 2.03mL |
40.62mL 8.12mL 4.06mL |
| 参考文献 |
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