中文名 | 4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮 |
英文名 | TROXACITABINE |
别名 | 曲沙他滨 拉米夫定杂质I 拉米夫定杂质09 拉米夫定EP杂质I 拉夫米定EP杂质I 拉米夫定杂质I(EP) 4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮 4-氨基-1-((2S,4S)-2-(羟甲基)-1,3-二氧戊环-4-基)嘧啶-2(1H)-酮 |
英文别名 | CS-150 (-)-Occc (-)-Bch 204 TROXACITABINE Lamivudine Impurity I (Troxacitabine) 4-Amino-1-[(2S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]pyrimidin-2-one 4-amino-1-[(2S,4S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]-1,2-dihydropyrimidin-2-one TROXACITABINE,2(1H)-PYRIMIDINONE, 4-AMINO-1-(2-(HYDROXYMETHYL)-1,3-DIOXOLAN-4-YL)-, (2S-CIS)- |
CAS | 145918-75-8 |
EINECS | 200-258-5 |
化学式 | C8H11N3O4 |
分子量 | 213.19 |
密度 | 1.71±0.1 g/cm3(Predicted) |
熔点 | 176-177° |
沸点 | 422.5±55.0 °C(Predicted) |
比旋光度 | D25 -38.33° (c = 0.43 in MeOH). |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
酸度系数 | 14.83±0.10(Predicted) |
存储条件 | 2-8°C(protect from light) |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Off-White |
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. |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!