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4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮
产品纠错
CAS号:145918-75-8 | 英文名称:TROXACITABINE
分子式 C8H11N3O4
分子量 213
EINECS号 200-258-5
MDL MFCD00871100
Smiles
InChIKey
乙二醇化学百科
基本信息
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
英文名称 TROXACITABINE
CAS号 145918-75-8
分子式 C8H11N3O4
分子量 213.19
EINECS号 200-258-5
物化性质
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)
溶解度 可溶于DMSO(少许)、甲醇(少许)
形态 固体
酸度系数(pKa) 14.83±0.10(Predicted)
颜色 白色至类白色
稳定性 吸湿性
安全信息
生产及用途
Troxacitabine是一种具有强效抗肿瘤活性的二氧戊环类似物。

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.

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.

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