Irinotecan-hydrochloride-trihydrate-plus-Irinotecan-hydrochloride-trihydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIrinotecanhydrochloridetrihydrateCat.No.:HY-16568CASNo.:136572-09-3Synonyms:(+)-Irinotecanhydrochloridetrihydrate;CPT-11hydrochloridetrihydrate分⼦式:C₃₃H₄₅ClN₄O₉分⼦量:677.18作⽤靶点:Topoisomerase;Autophagy作⽤通路:CellCycle/DNADamage;Autophagy储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:50mg/mL(73.84mM;Needultrasonic)H2O:1.52mg/mL(2.24mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4767mL7.3836mL14.7671mL5mM0.2953mL1.4767mL2.9534mL10mM0.1477mL0.7384mL1.4767mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.69mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.69mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.5mg/mL(3.69mM);Clearsolution;NeedwarmingBIOLOGICALACTIVITY⽣物活性Irinotecanhydrochloridetrihydrate((+)-Irinotecanhydrochloridetrihydrate)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]。IC50&TargetTopoisomeraseI体外研究IrinotecanhydrochloridetrihydrateisatopoisomeraseIinhibitor.IrinotecaninhibitsthegrowthofLoVoandHT-29cells,withIC50sof15.8±5.1and5.17±1.4μM,respectively,andinducessimilaramountsofcleavablecomplexesinbothinLoVoandHT-29cells[2].Irinotecansuppressestheproliferationofhumanumbilicalveinendothelialcells(HUVEC),withanIC50of1.3μM[3].体内研究Irinotecan(CPT-11,5mg/kg)significantlyinhibitsthegrowthoftumorsbyintratumoralinjectiondailyfor5days,ontwoconsecutiveweeksinrats,andsucheffectsalsooccurviacontinuousintraperitonealinfusionbyosmoticminipumpintomice.However,Irinotecan(10mg/kg)showsnoeffectonthegrowthoftumorbyi.p[1].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[3].PROTOCOLCellAssay[2]Exponentiallygrowingcellsareseededin20cm2disheswithanoptimalcellnumberforeachcellline(20,000forLoVocells,100,000forHT-29cells).Theyaretreated2dayslaterwithincreasingconcentrationsofirinotecanorSN-38foronecelldoublingtime(24hforLoVocells,40hforHT-29cells).Afterwashingwith0.15MNaCl,thecellsarefurthergrownfortwodoublingtimesinnormalmedium,detachedfromthesupportwithtrypsin-EDTAandcountedinahemocytometer.TheIC50valuesarethenestimatedasthedrugconcentrationsresponsiblefor50%growthinhibitionascomparedwithcellsincubatedwithoutdrug[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalIrinotecanhasbeenadministeredbyintratumoralinjectionat0.1ccvolumeoftheappropriatesolution,foraAdministration[1]dosesof5mg/kgdailyfor5days,ontwoconsecutiveweeks,followedbya7-daysrestperiod,referredtoasonecycleoftherapy.Ratsreceivethreecyclesoveraperiodof8weeks.Controlanimalsreceive0.1ccofsterile0.9%sodiumchloridesolutionbyintratumoralinjectioninthesameruleofadministrationasthatof2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEanimalsofgroupII[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Cell.2022Sep1;185(18):3356-3374.e22.•SignalTransductTargetTher.2021May28;6(1):188.•CellDiscov.2022Sep14;8(1):92.•Gastroenterology.2021Nov;161(5):1601-1614.e23.•Biomaterials.16September2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MoralesC,etal.Antitumoraleffectofirinotecan(CPT-11)onanexperimentalmodelofmalignantneuroectodermaltumor.JNeurooncol.2002Feb;56(3):219-26.[2].PavillardV,etal.Determinantsofthecytotoxicityofirinotecanintwohumancolorectaltumorcelllines.CancerChemotherPharmacol.2002Apr;49(4):329-35.Epub2002Jan30.[3].AllegriniG,etal.Thrombospondin-1plusirinotecan:anovelantiangiogenic-chemotherapeuticcombinationthatinhibitsthegrowthofadvancedhumancolontumorxenograftsinmice.CancerChemotherPharmac