LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
性状
Solid
IC50 & Target[1][2]
Top1
体外研究(In Vitro)
The GI50 value of LMP744 (MJ-III-65) for NCI60 cells is 0.1 μM.LMP744 (0.1-5 μM, 3 days) induces dose-dependent accumulation of cells in the S and G2 phases of the cell cycle. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LMP744 (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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. 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.[2]. 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
溶解度数据
In Vitro: DMSO : 105 mg/mL (214.76 mM; Need ultrasonic)配制储备液