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Phosphorylase
/ Doxifluridine/去氧氟尿苷

Doxifluridine/去氧氟尿苷 {[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是一种胸苷激酶激活剂，作用于PC9-DPE2细胞，IC50为0.62 μM。

Doxifluridine/去氧氟尿苷 化学结构 CAS号：3094-09-5
Doxifluridine/去氧氟尿苷 化学结构
CAS号：3094-09-5
Doxifluridine/去氧氟尿苷 3D分子结构
CAS号：3094-09-5
Doxifluridine/去氧氟尿苷 化学结构 CAS号：3094-09-5
Doxifluridine/去氧氟尿苷 3D分子结构 CAS号：3094-09-5
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Doxifluridine/去氧氟尿苷 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 HCl ✔ 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/去氧氟尿苷 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/去氧氟尿苷 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/去氧氟尿苷 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/去氧氟尿苷 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/去氧氟尿苷 技术信息

CAS号3094-09-5
分子式C9H11FN2O5
分子量 246.19
SMILES Code C[C@@H]1[C@H]([C@H]([C@H](N2C(NC(C(F)=C2)=O)=O)O1)O)O
MDL No. MFCD00866530
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

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

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/去氧氟尿苷 纯度/质量文件 | Doxifluridine/去氧氟尿苷 亚型比较 | Doxifluridine/去氧氟尿苷 生物活性 | Doxifluridine/去氧氟尿苷 临床数据 | Doxifluridine/去氧氟尿苷 参考文献 | Doxifluridine/去氧氟尿苷 实验方案 | Doxifluridine/去氧氟尿苷 技术信息

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