Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELMP744hydrochlorideCat.No.:HY-U00248ACASNo.:308246-57-3Synonyms:MJ-III65hydrochloride;NSC706744hydrochloride分?式:C??H??ClN?O?分?量:488.92作?靶點:Topoisomerase作?通路:CellCycle/DNADamage儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:105mg/mL(214.76mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0453mL10.2266mL20.4532mL5mM0.4091mL2.0453mL4.0906mL10mM0.2045mL1.0227mL2.0453mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性LMP744hydrochloride(MJ-III65hydrochloride)?種DNA嵌和劑，拓撲異構酶1(Top1)抑制劑，具有抗腫瘤活性。IC50&TargetTop11/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究TheGI50valueofLMP744(MJ-III-65)forNCI60cellsis0.1μM[2].LMP744(0.1-5μM,3days)inducesdose-dependentaccumulationofcellsintheSandG2phasesofthecellcycle[2].CellCytotoxicityAssay[2]CellLine:P388andP388Top1-deficientmurineleukemiacells.Concentration:0.1-100μMIncubationTime:3daysResult:Induceddose-dependentaccumulationofcellsintheSandG2phasesofthecellcycle.體內(nèi)研究LMP744(MJ-III-65)(10-50mg/kg)administeredi.v.pushonceaweekfor4weeksinnudemicemoderatelyactivesagainsthumanA253andFaDutumorxenograftswithoutsignificanttoxicity[1].AnimalModel:Athymicnudemice(nu/nu,female,20-25g,8-12weeksold)transplantedwithA253andFaDuhumanheadandneckxenografts[1].Dosage:10,25,or50mg/kg/week,4weeksAdministration:I.V.pushviatailveinResult:ModeratelyactivedagainsthumanA253andFaDutumorxenograftswithoutsignificanttoxicity.REFERENCES[1].AntonyS,etal.CellulartopoisomeraseIinhibitionandantiproliferativeactivitybyMJ-III-65(NSC706744),anindenoisoquinolinetopoisomeraseIpoison.MolPharmacol.2005Feb;67(2):523-30.[2].AntonyS,etal.Bisindenoisoquinolinebis-1,3-{(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino}propanebis(trifluoroacetate)(NSC727357),aDNAintercalatorandtopoisomeraseinhibitorwithantitumoractivity.MolPharmacol.2006McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear