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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEtoposideCat.No.:HY-13629CASNo.:33419-42-0Synonyms:VP-16;VP-16-213分?式:C??H??O??分?量:588.56作?靶點(diǎn):Topoisomerase;Autophagy;Mitophagy;Bacterial;Apoptosis;Antibiotic作?通路:CellCycle/DNADamage;Autophagy;Anti-infection;Apoptosis儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥39mg/mL(66.26mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6991mL8.4953mL16.9906mL5mM0.3398mL1.6991mL3.3981mL10mM0.1699mL0.8495mL1.6991mL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(protectfromlight)。-80°C儲存時(shí),請?jiān)?個(gè)?內(nèi)使?,-20°C儲存時(shí),請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(shí)驗(yàn)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑:1%DMSO>>99%salineSolubility:≥0.5mg/mL(0.85mM);Clearsolution2.請依序添加每種溶劑:10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.25mM);Clearsolution3.請依序添加每種溶劑:10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.25mM);Clearsolution4.請依序添加每種溶劑:5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.25mM);Clearsolution5.請依序添加每種溶劑:5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.25mM);ClearsolutionBIOLOGICALACTIVITY?物活性Etoposide(VP-16;VP-16-213)?種常?的抗腫瘤化療劑。Etoposide抑制拓?fù)洚悩?gòu)酶II(topoisomerase-II),從?抑制DNA復(fù)制。Etoposide誘導(dǎo)細(xì)胞周期停滯,凋亡(apoptosis)和?噬(autophagy)。IC50&TargetTopoisomeraseII體外研究Etoposideiscapableofcausingcytotoxicityonpancreaticβ-cellsbyinducingapoptosisthroughtheJNK/ERK-mediatedGSK-3downstream-triggeredmitochondria-dependentsignalingpathwayinRIN-m5Fcells[1].EtoposideandAnti-HumanVEGFsignificantlyabolishP1sphere-formingability,aneffectassociatedwithapoptosisofthissubsetofcells[2].Etoposidephosphate(0-1μM;72hours)inhibitsHCT116FBXW+/+,FBXW-/-andp53-/-asadose-dependentmanner,exhibitsIC50sof0.945μM;0.375μM;and1.437μM,respectively[5].Etoposide(25μM;6hours)delaysp53recoverinFBXW7-deficientcells.Inaddition,FBXW7expressionisdisappearedinFBXW7-/-cells[5].CellViabilityAssay[5]CellLine:HCT116FBXW+/+,FBXW-/-andp53-/-cellsConcentration:0.025μM,0.05μM,0.075μM,0.1μM,0.2μM,0.4μM,0.6μM,0.8μM,1μMIncubationTime:72hoursResult:InhibitsHCT116FBXW+/+p>,FBXW-/-andp53-/-cellgrowthasaconcentrationmanner.WesternBlotAnalysis[5]CellLine:HCT116FBXW7+/+orFBXW7-/-cellsConcentration:25μMIncubationTime:6hoursResult:Exhibitedthattherecoveryofp53levelsafterDNAdamageismediatedbyFBXW7.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究Etoposide(50μM)andAnti-HumanVEGF-treatedhypoxiccellsinjectedintravenouslyintoimmunodeficientmicerevealsareducedcapacitytoinducelungcolonies,whichalsoappearwithalongerlatencyperiod[2].Etoposide(10mg/kg/day,i.v.)withNSC109724andNSC241240,reducesthetumorvolumeinthehepatoblastomacellinjectedNMRInudemice[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Immunity.2022Aug9;55(8):1370-1385.e8.?AdvSci(Weinh).2020Sep28;7(21):2001364.?JExtracellVesicles.2022Apr;11(4):e12206.?Hepatology.2020May;71(5):1660-1677.?ProteinCell.2022Jan;13(1):47-64.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LeeKI,etal.Etoposideinducespancreaticβ-cellscytotoxicityviatheJNK/ERK/GSK-3signaling-mediatedmitochondria-dependentapoptosispathway.ToxicolInVitro.2016Jul26.pii:S0887-2333(16)30147-3.[2].CalvaniM,detal.Etoposide-Anti-HumanVEGFanewstrategyagainsthumanmelanomacellsexpressingstem-liketraits.Oncotarget.2016Jun9.doi:10.18632/oncotarget.9939.[3].Fuchs,J.,etal.ComparativeactivityofNSC119875,NSC109724,NSC123127,NSC241240,andetoposideinheterotransplantedhepatoblastoma.Cancer,1998.83(11):p.2400-7.[4].HandeKR,etal.TheImportanceofDrugSchedulinginCancerChemotherapy:EtoposideasanExample.Oncologist.1996;1(4):234-239.[5].CuiD,etal.FBXW7ConfersRadiationSurvivalbyTargetingp53forDegradation.CellRep.2020Jan14;30(2):

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