CamptothecinDescription
CamptothecinisatopoIpoisonthatbothinhibitsenzymeactivityandstABIlizesformationoftopoIcleavagecomplexes(HsiangetalJ.Biol.Chem.260:14873-14878,1985). TopoGENprovidesthisreagentasacontrolinhibitor/poisonoftopoisomeraseI. Forinvitrocleavagedetection,werecommendthatthedrugbetestedintherange100uM;however,cleavagesarestronglyinfluencedbytheamountoftopoisomeraseinthereactionaswellasthetypeofassaybeingemployed(SDS-K+vs.RADIoactiveEndLabeledDNAvs.testingforplasmidnick-ing). Notethatlargeramountsofenzymewillberequiredtodetectcleavagecomplex,comparedtoassaysthatmeasurecatalyticactivity. ThisisbecausecleavageassaysarestoichiometricbasedassaysthatconsumetopoI.

ChemicalName:(S)-4-Ethyl-4,10-dihydroxy-1H-pyrano[3',4':6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)-dione

MolecularFormula:C20H16N2O4

MolecularWeight: 348.35

 

VialContents:
TG4110containslyophilizedCamptothecin. Additionof0.25mlofsolventtodrydrug(methanolorDMSO)willyieldaworkingstockof10mM. Insomecases,thedrugissuppliedalreadysUSPendedinDMSOat10mM(0.25ml)andisreadyforuse. Thedrugispre-testedandshowntoinducetopoIcleavagesusingpurifiedhumanTopoisomeraseIfromTopoGEN,Inc.

 

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