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Troxacitabine (BCH 4556)

Troxacitabine (BCH 4556) 是具有有效抗癌活性的核苷类似物。

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  • 货号: ajcx13140
  • CAS: 145918-75-8
  • 别名: 4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮,BCH 4556; L-OddC; SPD 758
  • 分子式: C8H11N3O4
  • 分子量: 213.19
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

Troxacitabine is nucleoside analog with potent anticancer activity.


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 IC50s range from 15-35 μM[1][2].


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[3]. 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[2].


[1]. Gourdeau H, et al. Antitumor activity of troxacitabine (Troxatyl) against anthracycline-resistant human xenografts. Cancer Chemother Pharmacol. 2002 Dec;50(6):490-6. [2]. Kadhim SA, et al. Potent antitumor activity of a novel nucleoside analogue, BCH-4556 (beta-L-dioxolane-cytidine), in human renal cell carcinoma xenograft tumor models. Cancer Res. 1997 Nov 1;57(21):4803-10. [3]. Weitman S, et al. The new dioxolane, (-)-2'-deoxy-3'-oxacytidine (BCH-4556, troxacitabine), has activity againstpancreatic human tumor xenografts. Clin Cancer Res. 2000 Apr;6(4):1574-8.

Protocol

Animal experiment:

Mice[3]Troxacitabine is administered i.v. to the animals at doses of 10 and 25 mg/kg on a daily 3 5 regimen. Gemcitabine is used as a positive control. The end points for the study included tumor growth inhibition (TGI), final weight, and the number of partial and complete tumor responses in the animals[3].

参考文献:

[1]. Gourdeau H, et al. Antitumor activity of troxacitabine (Troxatyl) against anthracycline-resistant human xenografts. Cancer Chemother Pharmacol. 2002 Dec;50(6):490-6.
[2]. Kadhim SA, et al. Potent antitumor activity of a novel nucleoside analogue, BCH-4556 (beta-L-dioxolane-cytidine), in human renal cell carcinoma xenograft tumor models. Cancer Res. 1997 Nov 1;57(21):4803-10.
[3]. Weitman S, et al. The new dioxolane, (-)-2'-deoxy-3'-oxacytidine (BCH-4556, troxacitabine), has activity againstpancreatic human tumor xenografts. Clin Cancer Res. 2000 Apr;6(4):1574-8.

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