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145918-75-8

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 145918-75-8
分子式 C8H11N3O4
分子量 213.19
MOL 文件 145918-75-8.mol
更新日期 2023/03/20 15:41:19
145918-75-8 结构式 145918-75-8 结构式

基本信息

中文别名
曲沙他滨
拉米夫定杂质I
拉米夫定杂质09
拉夫米定EP杂质I
拉米夫定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
英文别名
CS-150
L-Oddc
SPD 758
Bch 4556
(-)-Occc
Troxatyl
(-)-Bch 204
TROXACITABINE
α-L-Dioxolane-C
Lamivudine Impurity I
所属类别
生物化工:激动剂抑制剂

物理化学性质

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)
储存条件Keep in dark place,Sealed in dry,2-8°C
溶解度可溶于DMSO(少许)、甲醇(少许)
酸度系数(pKa)14.83±0.10(Predicted)
形态固体
颜色白色至灰白色
稳定性吸湿性

常见问题列表

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.

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