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CAS RN: 103766-25-2 | Product Number: C2243
Gimeracil
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Purity: >98.0%(T)(HPLC)
Synonyms:
- 5-Chloro-2,4-dihydroxypyridine
- 5-Chloro-2,4-pyridinediol
- 5-Chloro-4-hydroxy-2(1H)-pyridinone
Product Documents:
| Size | Unit Price | Same Day | 2-3 Business Days | Other Lead Time |
Shipping Information
|
|---|---|---|---|---|---|
| 1G |
NT$1,470
|
5 | 3 | It can be shipped in about 2 weeks after ordering | |
| 5G |
NT$4,998
|
13 | 1 | It can be shipped in about 2 weeks after ordering |
* The above prices include freight cost, customs, and other charges to the destination except for products that need to be shipped by sea or dry ice. For details, please contact
our distributor
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* The storage conditions are subject to change without notice.
| Product Number | C2243 |
| Purity / Analysis Method | >98.0%(T)(HPLC) |
| Molecular Formula / Molecular Weight | C__5H__4ClNO__2 = 145.54 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature | Room Temperature (Recommended in a cool and dark place, <15°C) |
| Packaging and Container | 1G-Glass Bottle with Plastic Insert (View image) |
| CAS RN | 103766-25-2 |
| Reaxys Registry Number | 119489 |
| PubChem Substance ID | 87560206 |
| SDBS (AIST Spectral DB) | 52168 |
| MDL Number | MFCD08458352 |
Specifications
| Appearance | White to Almost white powder to crystal |
| Purity(HPLC) | min. 98.0 area% |
| Purity(Neutralization titration) | min. 98.0 % |
| NMR | confirm to structure |
Properties (reference)
| Melting Point | 274 °C(dec.) |
GHS
Related Laws:
Transport Information:
| H.S.code* | 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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