Tegafur
产品说明书
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同义名 : | 替加氟 ;FT 207;NSC 148958;Abbreviation: UFT.;Uracil Foreign brand name: Uftoral;Uracil and Tegafur;Uracil and Ftorafur;oral fluorouraciluracil;TS-1;Ftorafur;5-Fluoro-1-(tetrahydro-2-furfuryl)uracil |
| CAS号 : | 17902-23-7 | |
| 货号 : | A332760 | |
| 分子式 : | C8H9FN2O3 | |
| 纯度 : | 98% | |
| 分子量 : | 200.167 | |
| MDL号 : | MFCD00012351 | |
| 存储条件： |
Pure form Sealed in dry,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(249.79 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(99.92 mM) |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tegafur is a prodrug of the antineoplastic agent fluorouracil, and is administered in a 1:4 molar ratio with the fluorouracil modulator uracil. Oral tegafur/uracil was associated with a significantly more favourable tolerability profile than IV fluorouracil in the two large randomised trials[3]. The multifunctional prodrugs of tegafur display selectivity toward cancer cells, antiangiogenic activity, and anticancer activities in vitro and in vivo, superior to those of tegafur[4]. Uracil-tegafur (UFT) is an oral anticancer drug containing uracil and 5‑fluorouracil prodrug tegafur and is widely used for adjuvant chemotherapy of colorectal cancer[5]. Uracil plus tegafur was shown to be less toxic than the drug alone in all the species, and uracil was found to decrease the toxicity of tegafur. Administration of uracil with tegafur prevents the side effects of the drug on the heart and CNS by inhibiting the degradation of 5-fluorouracil[6]. The interspecies variations were observed in the enantioselective pharmacokinetics of FT(Tegafur), and the in-vivo enantioselectivity could be extrapolated from the in-vitro metabolic activities[7]. | ||
| 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 |
| NCT03129256 | Non-small Cell Lung Cancer | Phase 2 | Recruiting | December 31, 2019 | China, Jiangsu ... 展开 >> Changzhou Cancer Hospital of Soochow University Recruiting Changzhou, Jiangsu, China, 213000 Contact: Tong Zhou, Dr. +86-15861153525 Principal Investigator: Tong Zhou, Dr. 收起 << |
| NCT02623153 | Gastric Cancer | Phase 2 | Not yet recruiting | December 2019 | - |
| NCT03195881 | - | Recruiting | April 30, 2019 | United States, Ohio ... 展开 >> Bethesda North TriHealth Hospital Recruiting Cincinnati, Ohio, United States, 45242 Contact: Jocelyn LaMar, BS 513-865-5072 Jocelyn_LaMar@trihealth.com 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
5.00mL 1.00mL 0.50mL |
24.98mL 5.00mL 2.50mL |
49.96mL 9.99mL 5.00mL |
| 参考文献 |
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[3]Wellington K, Goa KL. Oral tegafur/uracil. Drugs Aging. 2001;18(12):935-48; discussion 949-50 |