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其他
Phosphorylase
/ Doxifluridine

去氧氟尿苷 /Doxifluridine {[allProObj[0].p_purity_real_show]}

货号：A137458 同义名： 5'-脱氧-5-氟尿苷 / 5'-DFUR;5-Fluoro-5'-deoxyuridine

Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.

Doxifluridine 化学结构 CAS号：3094-09-5
Doxifluridine 化学结构
CAS号：3094-09-5
Doxifluridine 3D分子结构
CAS号：3094-09-5
Doxifluridine 化学结构 CAS号：3094-09-5
Doxifluridine 3D分子结构 CAS号：3094-09-5
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Doxifluridine 纯度/质量文件 产品仅供科研

货号：A137458 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Phosphorylase ↓ 其他靶点 纯度
Tipiracil hydrochloride ✔ 98%
CP-91149 +++

Glycogen phosphorylase (GP), IC50: 0.13 μM

 		98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Doxifluridine 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].

Doxifluridine 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 <<

Doxifluridine 参考文献

[1]Metronomic doxifluridine chemotherapy combined with the anti-angiogenic agent TNP-470 inhibits the growth of human uterine carcinosarcoma xenografts

[2]Berne M, Gustavsson B, et al. Inhibition of thymidylate synthase after administration of doxifluridine in a transplantable colon carcinoma in the rat. Cancer Invest. 1988;6(4):377-83.

Doxifluridine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.06mL

0.81mL

0.41mL

20.31mL

4.06mL

2.03mL

40.62mL

8.12mL

4.06mL

Doxifluridine 技术信息

CAS号3094-09-5
分子式C9H11FN2O5
分子量 246.192
别名 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
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
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
动物实验配方

Tags: Doxifluridine | 3094-09-5 | Ro 21-9738 | 5-Fluoro-5'-deoxyuridine | 5'-DFUR | Nucleoside Antimetabolite/Analog Inhibitor | Apoptosis | Thymidylate Synthase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Doxifluridine 纯度/质量文件 | Doxifluridine 亚型比较 | Doxifluridine 生物活性 | Doxifluridine 临床数据 | Doxifluridine 参考文献 | Doxifluridine 实验方案 | Doxifluridine 技术信息

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