LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].
The GI50 value of LMP744 (MJ-III-65) for NCI60 cells is 0.1 μM[1].LMP744 (0.1-5 μM, 3 days) induces dose-dependent accumulation of cells in the S and G2 phases of the cell cycle[1].|| Cell Cytotoxicity Assay[1]||Cell Line:|P388 and P388 Top1-deficient murine leukemia cells|Concentration:|0.1-100 μM|Incubation Time:|3 days|Result:|induced dose-dependent accumulation of cells in the S and G2 phases of the cell cycle
MJ-III-65 (10-50 mg/kg) administered i.v. push once a week for 4 weeks in nude mice moderately actives against human A253 and FaDu tumor xenografts without significant toxicity[2].|| Animal Model:|Athymic nude mice (nu/nu, female, 20-25 g, 8-12 weeks old) transplanted with A253 and FaDu human head and neck xenografts[2].|Dosage:|10, 25, or 50 mg/kg/week, 4 weeks|Administration:|i.v. push via tail vein|Result:|moderately actived against human A253 and FaDu tumor xenografts without significant toxicity
[1]. Antony S, et al. Bisindenoisoquinoline bis-1,3-{( 5,6-dihydro-5,11-diketo-11H-indeno [1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity. Mol Pharmacol. 2006 Sep;70(3):1109-20. [2]. Antony S, et al. Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison. Mol Pharmacol. 2005 Feb;67(2):523-30.