Irinotecan(CPT-11)Description
Irinotecan(alsoknownasCPT-11)isawatersoluble,semi-syntheticanalogueof20(S)camptothecin(CPT)withpromisingactivityagainstarangeoftumourtypes. IrinotecancausescelltoxicitybystABIlizingaternarycomplexbetweenthenuclearenzymetopoisomeraseI(topoI)anddouble-strandedDNA,leADIngtosingleanddoublestrandbreaks.[ClinExpPharmacolPhysiol.1996Oct-Nov;23(10-11):1000-4.] TopoGENprovidesthisreagentasacontrolpoison/inhibitoroftopoisomeraseI. Forinvitrocleavagedetection,werecommendthatthedrugbetestedoverawiderangeofuMconcentrations;however,cleavagesarestronglyinfluencedbytheamountoftopoisomeraseinthereactionaswellasthetypeofassaybeingemployed(SDSK+vs.RadioactiveEndLabeledDNAvs.testingforplasmidcleavages). Notethatlargeamountsofenzymewillberequiredtodetectcleavagecomplex,comparedtoassaysthatmeasurecatalyticactivity.
MolecularFormula:C33H38N4O6.HCl.3H2O
MolecularWeight:677.2
VialContents:
TG4101issuppliedalreadysUSPendedinwaterat10mM(0.25ml)andisreadyforuse.Thedrugispre-testedandshowntoinducetopocleavagesusingpurifiedhumantopoisomerasefromTopoGEN.