| CAS NO: | 103766-25-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 询价 |
| 500mg | 询价 |
| 1g | 询价 |
| 2g | 询价 |
| 5g | 询价 |
| 10g | 询价 |
| Molecular Weight (MW) | 145.54 |
|---|---|
| Formula | C5H4ClNO2 |
| CAS No. | 103766-25-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 29 mg/mL (199.3 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name: 5-chloro-2-hydroxypyridin-4(1H)-one InChi Key: ZPLQIPFOCGIIHV-UHFFFAOYSA-N InChi Code: InChI=1S/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9) SMILES Code: O=C1C=C(O)NC=C1Cl |
| Synonyms | Gimestat, chlorodihydroxypyridine; CDHP; Gimeracil |
| In Vitro | In vitro activity: Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks. Tail moments in neutral comet assay increased in gimeracil-treated cells. Gimeracil restrained the formation of foci of Rad51 and replication protein A (RPA), whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2. Gimeracil did not sensitize DPYD-depleted cells. Gimeracil inhibited DNA DSB repair. It did not sensitize cells deficient in HR but sensitized those deficient in NHEJ. In SCneo assay, Gimeracil reduced the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1. Kinase Assay: Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination. Cell Assay: Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks. Tail moments in neutral comet assay increased in gimeracil-treated cells. Gimeracil restrained the formation of foci of Rad51 and replication protein A (RPA), whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2. Gimeracil did not sensitize DPYD-depleted cells. Gimeracil inhibited DNA DSB repair. It did not sensitize cells deficient in HR but sensitized those deficient in NHEJ. In SCneo assay, Gimeracil reduced the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Oncol Rep. 2010 Nov;24(5):1307-13; Cancer Sci. 2011 Sep;102(9):1712-6 |
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