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145918-75-8

中文名稱 4-氨基-1-[(2S)-2-(羥甲基)-1,3-二氧雜環(huán)戊-4-基]嘧啶-2-酮
英文名稱 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 2024/10/08 11:41:43
145918-75-8 結(jié)構(gòu)式 145918-75-8 結(jié)構(gòu)式

基本信息

中文別名
曲沙他濱
拉米夫定雜質(zhì)I
拉米夫定雜質(zhì)09
拉夫米定EP雜質(zhì)I
拉米夫定EP雜質(zhì)I
拉米夫定雜質(zhì)I(EP)
4-氨基-1-[(2S)-2-(羥甲基)-1,3-二氧雜環(huán)戊-4-基]嘧啶-2-酮
英文別名
CS-150
L-Oddc
SPD 758
Bch 4556
(-)-Occc
Troxatyl
(-)-Bch 204
TROXACITABINE
α-L-Dioxolane-C
Lamivudine Impurity I
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點176-177°
比旋光度D25 -38.33° (c = 0.43 in MeOH).
沸點422.5±55.0 °C(Predicted)
密度1.71±0.1 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度可溶于DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)14.83±0.10(Predicted)
形態(tài)固體
顏色白色至灰白色
穩(wěn)定性吸濕性

常見問題列表

生物活性
Troxacitabine是一種具有強效抗腫瘤活性的二氧戊環(huán)類似物。
體外研究

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.

體內(nèi)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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