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CAS RN: 103766-25-2 | 产品编码: C2243
Gimeracil
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| 产品编码 | C2243 |
| 纯度/分析方法 | >98.0%(T)(HPLC) |
| 分子式/分子量 | C__5H__4ClNO__2 = 145.54 |
| 外观与形状（20°C） | 固体 |
| 储存温度 | 室温 (15°C以下阴凉干燥处) |
| 包装和容器 | 1G-Glass Bottle with Plastic Insert （查看图片） |
| CAS RN | 103766-25-2 |
| Reaxys-RN | 119489 |
| PubChem物质ID | 87560206 |
| SDBS (AIST Spectral DB) | 52168 |
| MDL编号 | MFCD08458352 |
技术规格
| Appearance | White to Almost white powder to crystal |
| Purity(HPLC) | min. 98.0 area% |
| Purity(Neutralization titration) | min. 98.0 % |
| NMR | confirm to structure |
物性（参考值）
| 熔点 | 274 °C(dec.) |
GHS
相关法规
运输信息
| HS编码* | 2933.39-000 |
应用
Gimeracil: A Dihydropyrimidine Dehydrogenase (DPD) Inhibitor
Gimeracil (5-chloro-2,4-dihydroxypyridine or CDHP) is a potent inhibitor of dihydropyrimidine dehydrogenase (DPD) which is an enzyme that is involved in pyrimidine degradation. Gimeracil itself does not influence cell proliferation, whereas it reversibly inhibits 5-FU [F0151] degradation and enhanced 5-FU cytotoxicity in tumor cell lines. Gimeracil is often used as combined agents to enhance the antitumor activity of fluoropyrimidines, such as S-1 (tegafur [F0635] a prodrug of 5-FU, gimeracil and potassium oxonate [O0164] at a molar ratio of 1:0.4:1). (The product is for research purpose only.)
References
- Inhibitory effects of pyrimidine, barbituric acid and pyridine derivatives on 5-fluorouracil degradation in rat liver extracts
- Development of a novel form of an oral 5-fluorouracil derivative (S-1) directed to the potentiation of the tumor selective cytotoxicity of 5-fluorouracil by two biochemical modulators
- Antitumor activity of 1 M tegafur-0.4 M 5-chloro-2,4-dihydroxypyridine-1 M potassium oxonate (S-1) against human colon carcinoma orthotopically implanted into nude rats
- Enhancement of the antitumor activity of 5-fluorouracil (5-FU) by inhibiting dihydropyrimidine dehydrogenase activity (DPD) using 5-chloro-2,4-dihydroxypyridine (CDHP) in human tumor cells
- CYP2A6 and the plasma level of 5-chloro-2,4-dihydroxypyridine are determinants of the pharmacokinetic variability of tegafur and 5-fluorouracil, respectively, in Japanese patients with cancer given S-1
参考文献
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