4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮

中文名称:

4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮

中文同义词:

4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮;曲沙他滨;拉米夫定杂质I(EP);拉米夫定EP杂质I;拉夫米定EP杂质I;拉米夫定杂质I;拉米夫定杂质09

英文名称:

TROXACITABINE

英文同义词:

TROXACITABINE;TROXACITABINE,2(1H)-PYRIMIDINONE, 4-AMINO-1-(2-(HYDROXYMETHYL)-1,3-DIOXOLAN-4-YL)-, (2S-CIS)-;4-Amino-1-[(2S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]pyrimidin-2-one;(-)-Bch 204;CS-150;Lamivudine Impurity I (Troxacitabine);4-amino-1-[(2S,4S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]-1,2-dihydropyrimidin-2-one;(-)-Occc

CAS号:

145918-75-8

分子式:

C8H11N3O4

分子量:

213.19

EINECS号:

200-258-5

相关类别:

对照品-杂质对照品;拉米夫定;杂质对照品

Mol文件:

145918-75-8.mol

熔点 

176-177°

比旋光度 

D25 -38.33° (c = 0.43 in MeOH).

沸点 

422.5±55.0 °C(Predicted)

密度 

1.71±0.1 g/cm3(Predicted)

储存条件 

Keep in dark place,Sealed in dry,2-8°C

酸度系数(pKa)

14.83±0.10(Predicted)

生物活性

Troxacitabine是一种具有强效抗肿瘤活性的二氧戊环类似物。

体外研究

Troxacitabine has shown cutotoxicity in cancer cell lines of hepatocellular (HepG2), prostate (PC3, DUI45), non-small cell lung (NCI-H460, NCr-322M) colon (HT29), renal (CAK-l, A498, RXF-393, SNI2-C) and pancreatic origin (Pnac-Ol, MiaPa Ca) with IC 50 s range from 15-35 μM.

体内研究

Troxacitabine is highly active against the Panc-01 model, with TGI levels of 88.5% and 84.3% at the 10 and 25 mg/kg doses, respectively. The mean final tumor weights for animals given troxacitabine are also significantly smaller compared with vehicle controls. Troxacitabine has less activity against the MiaPaCa model. Troxacitabine is very effective in human RCC tumor xenograft models, including CAM-i, A498, RXF-393, and SN12C carcinomas. Very good responses are ob served in animals bearing CAM-i, A498, and RXF-393 RCC tumors given i.p. doses of 10, 25, and 50 mg/kg twice a day for 5 days.