|Product Name||Ipragliflozin||CAS No.||761423-87-4|
|Molecular Weight||392.4||Molecular Formula||C22H20N2O5|
Active metabolite of CPT-11 that inhibits DNA topoisomerase I (IC 50 values are 0.74 and 1.9 μ M in P388 and Ehrlich cells respectively). Inhibits DNA and RNA synthesis (IC 50 values are 0.077 and 1.3 μ M respectively) but does not affect protein synthesis. Displays potent antitumor activity against a range of human tumor cell lines (IC 50 values are 3.3, 13, 19 and 22 nM for HCT-116, BEL-7402, HL60 and HELA cells respectively). The paper reported an investigation of the pharmacokinetics of SN-38 (7-Ethyl-10-Hydroxycamptothecin) in rats and the tissue distribution in mice after injection of irinotecan hydrochloride nanoparticles (CPT-11) via tail veins. An LC-MS/MS method was established to determine the concentrations of 7-Ethyl-10-Hydroxycamptothecin in whole blood of rats and in different tissues of mice. The pharmacokinetics and tissue distribution of 7-Ethyl-10-Hydroxycamptothecin were compared after the intravenous injection of CPT-11 NPs and CPT-11 solution. Compared with irinotecan solution, the elimination half-life of 7-Ethyl-10-Hydroxycamptothecin was prolonged from 2.17 h to 2.67 h after the intravenous injection of CPT-11 NPs, but its AUC had little change. After the injection of CPT-11 NPs in mice, over time, the concentrations of CPT-11-metabolized 7-Ethyl-10-Hydroxycamptothecin in CPT-11 NPs were significantly higher in the whole blood, colon and lungs than those in CPT-11 solution, followed by in the spleen and liver, but those in the heart and brain had no change. However, the amount of 7-Ethyl-10-Hydroxycamptothecin in the kidneys was reduced with time. CPT-11 NPs could prolong 7-Ethyl-10-Hydroxycamptothecin's (one of its metabolites) blood circulation time in rats and significantly increased the concentration of CPT-11-metabolized 7-Ethyl-10-Hydroxycamptothecin in the whole blood, colon and lungs of mice. CPT-11 NPs made 7-Ethyl-10-Hydroxycamptothecin efficiently target-bind to the colon and lungs of mice.
A metabolite of Irinotecan, a DNA topoisomerase inhibitor