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LMP744 hydrochloride

Names

[ CAS No. ]:
308246-57-3

[ Name ]:
LMP744 hydrochloride

[Synonym ]:
5H-[1,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione,6-[3-[(2-hydroxyethyl)amino]propyl]-2,3-dimethoxy-,monohydrochloride

Biological Activity

[Description]:

LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

[Target]

Top1[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]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H25ClN2O7

[ Molecular Weight ]:
488.91800

[ Exact Mass ]:
488.13500

[ PSA ]:
108.25000

[ LogP ]:
3.12370

[ Storage condition ]:
2-8℃

Related Compounds