Biological Activity
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].
In Vitro
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
In Vivo
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
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.