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CAS No. : 136572-09-3
MCE 国际站:Irinotecan hydrochloride trihydrate
产品活性:Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) 是一种拓扑异构酶 I (topoisomerase I) 抑制剂,可用于结肠癌和直肠癌的研究。
研究领域:Cell Cycle/DNA Damage | Autophagy
作用靶点:Topoisomerase | Autophagy
In Vitro: Irinotecan hydrochloride trihydrate is a topoisomerase I inhibitor. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC50s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC50 of 1.3 μM.
In Vivo: Irinotecan (CPT-11, 5 mg/kg) significantly inhibits the growth of tumors by intratumoral injection daily for 5 days, on two consecutive weeks in rats, and such effects also occur via continuous intraperitoneal infusion by osmotic minipump into mice. However, Irinotecan (10 mg/kg) shows no effect on the growth of tumor by i.p. Irinotecan (CPT-11, 100-300 mg/kg, i.p.) apparently suppresses tumor growth of HT-29 xenografts in athymic female mice by day 21. The two groups of Irinotecan (125 mg/kg) plus TSP-1 (10 mg/kg per day) or Irinotecan (150 mg/kg) in combination TSP-1 (20 mg/kg per day) are nearly equally effective and inhibit tumor growth 84% and 89%, respectively, and both are more effective than Irinotecan alone at doses of 250 and 300 mg/kg.
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