Irinotecan-hydrochloride-plus-Irinotecan-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIrinotecanhydrochlorideCat.No.:HY-16562ACASNo.:100286-90-6Synonyms:(+)-Irinotecanhydrochloride;CPT-11hydrochloride分?式:C??H??ClN?O?分?量:623.14作?靶點(diǎn):Topoisomerase;Autophagy作?通路:CellCycle/DNADamage;Autophagy儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(200.60mM;Needultrasonic)H2O:3.33mg/mL(5.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6048mL8.0239mL16.0478mL5mM0.3210mL1.6048mL3.2096mL10mM0.1605mL0.8024mL1.6048mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:10mg/mL(16.05mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.34mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.34mM);Clearsolution4.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.34mM);Clearsolution5.請依序添加每種溶劑：50%PEG300>>50%salineSolubility:10mg/mL(16.05mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Irinotecanhydrochloride((+)-Irinotecanhydrochloride)?種拓?fù)洚悩?gòu)酶I(topoisomeraseI)抑制劑，可?于結(jié)腸癌和直腸癌的研究[1]。IC50&TargetTopoisomeraseI體外研究IrinotecanhydrochlorideisatopoisomeraseIinhibitor.IrinotecaninhibitsthegrowthofLoVoandHT-29cells,withIC50sof15.8±5.1and5.17±1.4μM,respectively,andinducessimilaramountsofcleavablecomplexesinbothinLoVoandHT-29cells[2].Irinotecansuppressestheproliferationofhumanumbilicalveinendothelialcells(HUVEC),withanIC50of1.3μM[3].體內(nèi)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,fora2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAdministration[1]dosesof5mg/kgdailyfor5days,ontwoconsecutiveweeks,followedbya7-daysrestperiod,referredtoasonecycleoftherapy.Ratsreceivethreecyclesoveraperiodof8weeks.Controlanimalsreceive0.1ccofsterile0.9%sodiumchloridesolutionbyintratumoralinjectioninthesameruleofadministrationasthatofanimalsofgroupII[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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.CancerChemother