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CAS No. : 26599-17-7
MCE 国际站:Thiarabine
产品活性:Thiarabine (OSI-7836) 具有抗肿瘤活性,能抑制 DNA 的合成。
研究领域:Cell Cycle/DNA Damage
作用靶点:DNA/RNA Synthesis
In Vivo: Thiarabine has demonstrated exceptional antitumor activity against numerous human tumor xenografts in mice, being superior to gemcitabine, clofarabine, or cytarabine. Unlike cytarabine, Thiarabine demonstrates excellent activity against solid tumor xenografts, suggesting that this agent has the kind of robust activity in animal models that leads to clinical utility. Thiarabine is effective orally (bioavailability of approximately 16%) and with once per day dosing: Two characteristics that distinguish it from cytarabine. Although both the structure and basic mechanism of action of Thiarabine are similar to that of cytarabine, there are many quantitative differences in the biochemical pharmacology of these two agents that can explain the superior antitumor activity of Thiarabine. Two important attributes are the long retention time of the 5'-triphosphate of thiarabine in tumor cells and its potent inhibition of DNA synthesis. The biochemical pharmacology of Thiarabine is also different from that of gemcitabine.
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