Irinotecan (hydrochloride)

100286-90-6

C33H39ClN4O6

DMSO : >= 51 mg/mL (81.84 mM)

Cell Cycle/DNA Damage; Autophagy

Irinotecan hydrochloride is a water soluble topoisomerase I inhibitor with antitumor activity. IC50 & Target: Topoisomerase I^[1] In Vitro: Irinotecan hydrochloride 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 uM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells^[2]. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC₅₀ of 1.3 uM^[3]. 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^[1]. 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^[3].