10-HydroxyCamptothecinDescription
10-HydroxyCamptothecinhasshownpromisingactivityagainstarangeoftumourtypes. ThisCPTderivativecausescelltoxicitybystABIlizingaternarycomplexbetweenthenuclearenzymetopoisomeraseI(topoI)anddouble-strandedDNA,leADIngtosingleanddoublestrandbreaks.TopoGENprovidesthisreagentasacontrolpoison/inhibitoroftopoisomeraseI. Forinvitrocleavagedetection,werecommendthatthedrugbetestedoverawiderangeofuMconcentrations;however,cleavagesarestronglyinfluencedbytheamountoftopoisomeraseinthereactionaswellasthetypeofassaybeingemployed(SDSK+vs.Radioac-tiveEndLabeledDNAvs.testingforplasmidcleavages). Notethatlargeamountsofenzymewillberequiredtodetectcleavagecomplex,comparedtoassaysthatmeasurecatalyticactivity.
ChemicalName:(S)-4-Ethyl-4,10-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
MolecularFormula:C20H16N2O5
MolecularWeight:364
VialContents:
TG4103issuppliedalreadysUSPendedinDMSOat10mM(0.25ml)andisreadyforuse. Thedrugispre-testedandshowntoinducetopocleavagesusingpurifiedhumantopoisomerasefromTopoGEN.