ProductDescription
IrinotecanhydrochlorideisaninhibitorofTopoisomeraseI,andisisactivatedbyhydrolysistoSN-38(theactivemetaboliteofIrinotecan).
Irinotecanhydrochlorideisthehydrochloridesaltofasemisyntheticderivativeofcamptothecin,acytotoxic,quinoline-basedalkaloidextractedfromtheAsiantreeCamptothecaacuminata.Irinotecan,aprodrug,isconvertedtoaBIOLOGicallyactivemetabolite7-ethyl-10-hydroxy-camptothecin(SN-38)byacarboxylesterase-convertingenzyme.Onethousand-foldmorepotentthanitsparentcompoundirinotecan,SN-38inhibitstopoisomeraseIactivitybystABIlizingthecleavablecomplexbetweentopoisomeraseIandDNA,resultinginDNAbreaksthatinhibitDNAreplicationandtriggerapoptoticcelldeath.
IncreasingconcentrationsofIrinotecan(0.1,1,10,100,and1000渭g/mL)inhibitsthegrowthofallcelllinesinadose-dependentmanner.COLO-357cellsaremostsensitiveandHT29mostresistanttoIrinotecanintheMTTassayonincubationfor90min.TheIC50concentrationsare100,50,5.4,23and46渭g/mLIrinotecanforHT29,NMG64/84,COLO-357,MIAPaCa-2andPANC-1,respectively