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CAS RN: 103766-25-2 | 產品號碼: C2243
| 產品號碼 | C2243 |
純度/分析方法 
|
>98.0%(T)(HPLC) |
| 分子式 / 分子量 | C__5H__4ClNO__2 = 145.54 |
| 外觀與形狀（20°C） | Solid |
| 儲存條件
|
Room Temperature (Recommended in a cool and dark place, <15°C) |
| 包裝和容器
|
1G-Glass Bottle with Plastic Insert （閲覽圖片） |
| CAS RN | 103766-25-2 |
| Reaxys-RN | 119489 |
| PubChem Substance ID | 87560206 |
| SDBS (AIST Spectral DB) | 52168 |
| MDL編號 | MFCD08458352 |
產品規格
| Appearance | White to Almost white powder to crystal |
| Purity(HPLC) | min. 98.0 area% |
| Purity(Neutralization titration) | min. 98.0 % |
| NMR | confirm to structure |
性質
| 熔點 | 274 °C(dec.) |
GHS
相關法規
運輸資料
| HS編碼* | 2933.39-000 |
Application
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
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