吉莫斯特；吉美嘧啶；CAS:103766-25-

中文名称:

吉莫斯特

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;二氢嘧啶脱氢酶(DPYD)抑制剂(GIMERACIL);吉美嘧啶 吉莫斯特;吉莫斯特(吉美嘧啶)

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;小分子抑制剂;抗肿瘤;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;PYRIDINE;Antitumors for Research and Experimental Use;Biochemistry;Chloropyridines;Halopyridines;Intermediates Fine Chemicals;Pharmaceuticals;oncology;Anticancer;有机化学

Mol文件:

103766-25-2.mol

熔点 

274 °C

沸点 

255.1±40.0 °C(Predicted)

密度 

1.56±0.1 g/cm3(Predicted)

储存条件 

Refrigerator

酸度系数(pKa)

4.50±1.00(Predicted)

InChIKey

ZPLQIPFOCGIIHV-UHFFFAOYSA-N

CAS 数据库

103766-25-2(CAS DataBase Reference)

生物活性

Gimeracil是一种二氢脱氢酶的抑制剂，在双链断裂修复中，抑制早期同源重组。

靶点

Target Value Dihydropyrimidine dehydrogenase

Target

Value

Dihydropyrimidine dehydrogenase

体外研究

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.

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.

体内研究

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.

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.

用途 

抗癌药S-1组成成分之一，可抑制抗肿瘤药物替加氟的毒副作用

安全说明 

24/25

海关编码 

29337900