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抑制剂/激动剂
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/ Tegafur

替加氟 /Tegafur {[allProObj[0].p_purity_real_show]}

货号：A332760 同义名： 替加氟 / FT 207;NSC 148958

Tegafur是5-氟尿嘧啶（5-FU）的前药，用于治疗癌症。

Tegafur 化学结构 CAS号：17902-23-7
Tegafur 化学结构
CAS号：17902-23-7
Tegafur 3D分子结构
CAS号：17902-23-7
Tegafur 化学结构 CAS号：17902-23-7
Tegafur 3D分子结构 CAS号：17902-23-7
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Tegafur 纯度/质量文件 产品仅供科研

货号：A332760 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 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Oxolinic acid ✔ 98+%
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLM636-1298, IC50: 0.97 μM

BLMfull-length, IC50: 2.98 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 98%
Favipiravir ✔ 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

 		98%
SU056 +

YB-1, IC50: 1.73 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。

Tegafur 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].

Tegafur 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 <<

Tegafur 参考文献

[1]Zhuk R. Structure-activity relationship in Ftorafur (Tegafur) and related 5-FU prodrugs. Adv Exp Med Biol. 1998;431:677-80.

[2]Ron IG, Lotan A, et al. Advanced colorectal carcinoma: redefining the role of oral ftorafur. Anticancer Drugs. 1996 Aug;7(6):649-54.

[3]Wellington K, Goa KL. Oral tegafur/uracil. Drugs Aging. 2001;18(12):935-48; discussion 949-50

[4]Engel D, Nudelman A, Tarasenko N, Levovich I, Makarovsky I, Sochotnikov S, Tarasenko I, Rephaeli A. Novel prodrugs of tegafur that display improved anticancer activity and antiangiogenic properties. J Med Chem. 2008 Jan 24;51(2):314-23

[5]Kobuchi S, Ito Y, Takamatsu D, Sakaeda T. Circadian variations in the pharmacokinetics of the oral anticancer agent tegafur-uracil (UFT) and its metabolites in rats. Eur J Pharm Sci. 2018 Oct 15;123:452-458

[6]Yamamoto J, Haruno A, Yoshimura Y, Unemi N, Kunimune Y, Yamashita K, Morita K. Effect of coadministration of uracil on the toxicity of tegafur. J Pharm Sci. 1984 Feb;73(2):212-4

[7]Yamamiya I, Yoshisue K, Ishii Y, Yamada H, Yoshida K. Species variation in the enantioselective metabolism of tegafur to 5-fluorouracil among rats, dogs and monkeys. J Pharm Pharmacol. 2014 Dec;66(12):1686-97

Tegafur 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.00mL

1.00mL

0.50mL

24.98mL

5.00mL

2.50mL

49.96mL

9.99mL

5.00mL

Tegafur 技术信息

CAS号17902-23-7
分子式C8H9FN2O3
分子量 200.167
别名 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
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,Room Temperature
溶解方案

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)

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

Tags: Tegafur | 17902-23-7 | FT 207 | NSC 148958 | FT207 | FT-207 | NSC148958 | NSC 148958 | NSC-148958 | Cell Cycle/DNA Damage | Nucleoside Antimetabolite/Analog | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tegafur 纯度/质量文件 | Tegafur 亚型比较 | Tegafur 生物活性 | Tegafur 临床数据 | Tegafur 参考文献 | Tegafur 实验方案 | Tegafur 技术信息

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