| Bioactivity | Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD)[1][2]. | ||||||||||||
| Invitro | Gimeracil reduces the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1[1].Gimeracil may enhance the efficacy of radiotherapy through the suppression of HR-mediated DNA repair pathways[1].Gimeracil pretreatment significantly restrains the formation of radiation-induced foci of Rad51 and RPA, whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2[2]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | Gimeracil (2.5-25 mg/kg, orally) may inhibit the rapid repair of X-ray-induced DNA damage in tumors[3]. Animal Model: | ||||||||||||
| Name | Gimeracil | ||||||||||||
| CAS | 103766-25-2 | ||||||||||||
| Formula | C5H4ClNO2 | ||||||||||||
| Molar Mass | 145.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Masaru Takagi, et al. Gimeracil sensitizes cells to radiation via inhibition of homologous recombination. Radiother Oncol. 2010 Aug;96(2):259-66. [2]. Koh-Ichi Sakata, et al. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination. Cancer Sci. 2011 Sep;102(9):1712-6. [3]. Masakazu Fukushima, et al. Gimeracil, a component of S-1, may enhance the antitumor activity of X-ray irradiation in human cancer xenograft models in vivo. Oncol Rep. 2010 Nov;24(5):1307-13. |