| Name | GIMERACIL |
| Synonyms | CDHP gimestat GIMERACIL 5-chloropyridine-2,4-diol 5-Chloro-4-hydroxy-2-pyridone 5-Chloro-2,4-dihydroxypyridine 5-Chloro-4-hydroxy-2(1H)-pyridinone 2(1H)-Pyridinone, 5-chloro-4-hydroxy- 2(1H)-Pyridinone,5-chloro-4-hydroxy-(9CI) |
| CAS | 103766-25-2 |
| EINECS | 1312995-182-4 |
| InChI | InChI=1/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9) |
| InChIKey | ZPLQIPFOCGIIHV-UHFFFAOYSA-N |
| Molecular Formula | C5H4ClNO2 |
| Molar Mass | 145.54 |
| Density | 1.56±0.1 g/cm3(Predicted) |
| Melting Point | 274 °C |
| Boling Point | 255.1±40.0 °C(Predicted) |
| Flash Point | 124.3°C |
| Solubility | Soluble in DMSO (29 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ |
| Vapor Presure | 0.000408mmHg at 25°C |
| Appearance | solid |
| Color | White |
| pKa | 4.50±1.00(Predicted) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.617 |
| MDL | MFCD08458352 |
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| HS Code | 29337900 |
| Biological activity | Gimeracil is an inhibitor of dihydrogen dehydrogenase, which inhibits early homologous recombination in double-strand break repair. |
| Target | Value |
| Cell Line: | DLD-1, HeLa, and LC-11 cell lines. |
| Concentration: | 1 mM. |
| Incubation Time: | 48 h. |
| Result: | Inhibits the repair of irradiation-induced DNA double strand breaks. Did not increase the c-H2AX foci residual at 24 h in unirradiated cells. Exhibited anti-tumor activity. |
| Animal Model: | Nude mice (Lu-99, LC-11, KB/C3 and PAN-4 tumors were xenografted). |
| Dosage: | 2.5-25 mg/kg. |
| Administration: | Orally. |
| use | one of the S-1 components of anticancer drugs, which can inhibit the toxic and side effects of antitumor drugs tegafur |