9-AminoCamptothecinDescription
9-Amino-20-(R,S)-camptothecin(alsoknownas9-aminocampthecin)isananalogueofcamptothecin. LikeotherCPTcongeners,itshowssomepromisingactivityagainstarangeoftumortypes. ThiscompoundcausescelltoxicitybystABIlizingaternarycomplexbetweenthenuclearenzymetopoisomeraseI(topoI)anddouble-strandedDNA,leADIngtosingleanddoublestrandbreaks. TopoGENprovidesthisreagentasacontrolpoison/inhibitoroftopoisomeraseI. Forinvitrocleavagedetection,werecommendthatthedrugbetestedoverawiderangeofuMconcentrations;however,cleavagesarestronglyinfluencedbytheamountoftopoisomeraseinthereactionaswellasthetypeofassaybeingemployed(SDSK+vs.RadioactiveEndLabeledDNAvs.testingforplasmidcleavages). Notethatlargeamountsofenzymewillberequiredtodetectcleavagecomplex,comparedtoassaysthatmeasurecatalyticactivity.
MolecularFormula:C20H17N3O4
MolecularWeight:363.37
VialContents:
ThedrugissuppliedalreadysUSPendedinDMSOat10mM(0.25ml)andisreadyforuse. Thedrugispre-testedandshowntoinducetopocleavagesusingpurifiedhumantopoisomerasefromTopoGEN.