货号：I9162

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

rinotecan, a derivative of camptothecin improved in therapeutic efficacy, is a Topoisomerase I inhibitor with IC50 values of 1.32 μM and 1.53 μM for induction of formation of DNA-topoisomerase I cleavable complexes in LoVo cells and HT-29 cells, respectively. Irinotecan is effective on anti-proliferation against tumor cells, including vincristine- and Adriamycin-resistant P388 leukemia cells with IC50 values of 3μM and 9μM, respectively. Irinotecan at concentration of 30μM for 24h significantly increased the proportions significantly increased the proportions at the S and G2 /M phases of cell cycling and decreased population at the G1 phase in both Caco-2 and CW2 cells, but no apoptosis or necrosis observed. Irinotecan showed significant antitumor activity against a broad spectrum of experimental tumor models by i.p., i.v., or oral administration, including susceptible murine tumors SISO, Meth A fibrosarcoma, Lewis lung carcinoma, Ehrlich carcinoma, MH134 hepatoma, mammary carcinoma of C3H/HeN mice, LI 210, and P388 leukemia, at doses ranging in 25-800mg/kg, with low acute toxicity. The difference in efficacy of CPT-11 between species may be related to the metabolism of the drug, since CPT-11 is converted more efficiently into SN-38 in mice.

产品信息