吉莫斯特
中文名称 | 吉莫斯特 |
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中文同义词 | 吉莫斯特;吉莫斯特(CDHP);5-氯-2,4-二羟基吡啶;5-氯-4-羟基-2(1H)-吡啶酮;吉美嘧啶;吉美嘧啶 吉莫斯特;吉莫斯特(吉美嘧啶);吉莫斯特,5-氯-2,4-二羟基吡啶 |
英文名称 | Gimeracil |
英文同义词 | GIMERACIL;gimestat;5-Chloro-2,4-dihydroxypyridine;5-Chloro-4-hydroxy-2(1H)-pyridinone;5-Chloro-4-hydroxy-2-pyridone;2(1H)-Pyridinone,5-chloro-4-hydroxy-(9CI);5-chloropyridine-2,4-diol;2(1H)-Pyridinone, 5-chloro-4-hydroxy- |
CAS号 | 103766-25-2 |
分子式 | C5H4ClNO2 |
分子量 | 145.54 |
EINECS号 | 1312995-182-4 |
相关类别 | 精细化学品;代谢;抗肿瘤类;原料药;中间体;PYRIDINE;Antitumors for Research and Experimental Use;小分子抑制剂;抗肿瘤;Anticancer;医药 抗癌药物抑制剂中间体;细胞生物学试剂;药物杂质及中间体;医药原料药;有机化学;Biochemistry;Chloropyridines;Halopyridines;Intermediates & Fine Chemicals;Pharmaceuticals;oncology |
Mol文件 | 103766-25-2.mol |
结构式 |
吉莫斯特 性质
熔点 | 274 °C |
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沸点 | 255.1±40.0 °C(Predicted) |
密度 | 1.56±0.1 g/cm3(Predicted) |
储存条件 | Inert atmosphere,Store in freezer, under -20°C |
溶解度 | 溶于DMSO(高达5mg/ml)。 |
形态 | 固体 |
酸度系数(pKa) | 4.50±1.00(Predicted) |
颜色 | 白色 |
稳定性 | 可在-20°C的DMSO中的溶液下储存长达3个月。 |
InChIKey | ZPLQIPFOCGIIHV-UHFFFAOYSA-N |
CAS 数据库 | 103766-25-2(CAS DataBase Reference) |
Target | Value |
Dihydropyrimidine dehydrogenase |
Gimeracil reduces the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1.
Gimeracil may enhance the efficacy of radiotherapy through the suppression of HR-mediated DNA repair pathways.
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.
Cell Viability Assay
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. |
Gimeracil (2.5-25 mg/kg, orally) may inhibit the rapid repair of X-ray-induced DNA damage in tumors.
Animal Model: |
Nude mice (Lu-99, LC-11, KB/C3 and PAN-4 tumors were xenografted).
|
Dosage: | 2.5-25 mg/kg. |
Administration: | Orally. |
Result: | Exhibited anti-tumor activity. |
安全信息
安全说明 | 24/25 |
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海关编码 | 29337900 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-17469 | 吉莫斯特 Gimeracil | 103766-25-2 | 25mg | 550元 |
2024/08/19 | HY-17469 | 吉莫斯特 Gimeracil | 103766-25-2 | 10mM * 1mLin DMSO | 605元 |