Irinotecan-d5-hydrochloride-plus-Irinotecan-d-sub-5-sub-hydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEIrinotecan-d5hydrochlorideCat.No.:HY-16562ASCASNo.:718612-73-8Synonyms:(+)-Irinotecan-d5hydrochloride;CPT-11-d5hydrochloride;VAL-413-d5分子式:C₃₃H₃₄D₅ClN₄O₆分子量:628.17作用靶点:Autophagy;Topoisomerase;Isotope-LabeledCompounds作用通路:Autophagy;CellCycle/DNADamage;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Irinotecan-d5hydrochloride是氘代标记的Irinotecanhydrochloride(HY-16562A)。Irinotecanhydrochloride((+)-Irinotecanhydrochloride)是一种拓扑异构酶I(topoisomeraseI)抑制剂，可用于结肠癌和直肠癌的研究[1]。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].IrinotecanhydrochlorideisatopoisomeraseIinhibitor.IrinotecaninhibitsthegrowthofLoVoandHT-29cells,withIC50sof15.8±5.1and5.17±1.4μM,respectively,andinducessimilaramountsofcleavablecomplexesinbothinLoVoandHT-29cells[3].Irinotecansuppressestheproliferationofhumanumbilicalveinendothelialcells(HUVEC),withanIC50of1.3μM[4].体内研究Irinotecanhydrochloride(CPT-11hydrochloride,5mg/kg)significantlyinhibitsthegrowthoftumorsbyintratumoralinjectiondailyfor5days,ontwoconsecutiveweeksinrats,andsucheffectsalsooccurviacontinuousintraperitonealinfusionbyosmoticminipumpintomice.However,Irinotecan(10mg/kg)showsnoeffectonthegrowthoftumorbyi.p[2].Irinotecan(CPT-11,100-300mg/kg,i.p.)apparentlysuppressestumorgrowthofHT-29xenograftsinathymicfemalemicebyday21.ThetwogroupsofIrinotecan(125mg/kg)plusTSP-1(10mg/kgperday)orIrinotecan(150mg/kg)incombinationTSP-1(20mg/kgperday)arenearlyequallyeffectiveandinhibittumorgrowth84%and89%,respectively,andbotharemoreeffectivethanIrinotecanaloneatdosesof250and300mg/kg[4].1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEREFERENCESMoralesC,etal.Antitumoraleffectofirinotecan(CPT-11)onanexperimentalmodelofmalignantneuroectodermaltumor.JNeurooncol.2002Feb;56(3):219-26.PavillardV,etal.Determinantsofthecytotoxicityofirinotecanintwohumancolorectaltumorcelllines.CancerChemotherPharmacol.2002Apr;49(4):329-35.Epub2002Jan30.AllegriniG,etal.Thrombospondin-1plusirinotecan:anovelantiangiogenic-chemotherapeuticcombinationthatinhibitsthegrowthofadvancedhumancolontumorxenograftsinmice.CancerChemotherPharmacol.2004Mar;53(3):261-6.Epub2003Dec5.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi