MLN8054-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMLN8054Cat.No.:HY-10180CASNo.:869363-13-3分?式:C??H??ClF?N?O?分?量:476.86作?靶點(diǎn):AuroraKinase作?通路:CellCycle/DNADamage;Epigenetics儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:30mg/mL(62.91mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0971mL10.4853mL20.9705mL5mM0.4194mL2.0971mL4.1941mL10mM0.2097mL1.0485mL2.0971mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)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(dòng)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(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.36mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.24mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.36mM);ClearsolutionBIOLOGICALACTIVITY?物活性MLN8054?效，選擇性，有?服活性的極光激酶(auroraA)抑制劑，IC50值為4nM。IC50&TargetAuroraA4nM(IC50)體外研究MLN8054isanATP-competitive,reversibleinhibitorofrecombinantAuroraAkinase.MLN8054is>40-foldmoreselectiveforAuroraAcomparedwiththefamilymemberAuroraB.MLN8054selectivelyinhibitsAuroraAoverAuroraBinculturedhumantumorcells.MLN8054treatmentresultsinG2/Maccumulationandspindledefectsandinhibitsproliferationinmultipleculturedhumantumorcellslines.MLN8054effectivelyinhibitsthegrowthofcellsfromdiversetissueoriginswithIC50valuesrangingfrom0.11to1.43μM[1].TreatmentofhumantumorcellsgrowninculturewithMLN8054showsanumberofmorphologicandbiochemicalchangesassociatedwithsenescence[2].體內(nèi)研究IntheHCT-116tumor-bearingmice,MLN8054treatmentinhibitstumorgrowthdosedependently.MLN8054isgenerallywelltolerated.MLN8054alsoinhibitsthegrowthofthePC-3tumorxenograftinnudemice.MLN8054TreatmentResultsinInhibitionofAuroraA,AccumulationofMitoticCells,andApoptosisinvivo[1].MLN8054selectivelyinhibitsAuroraAkinaseactivitywhendosedat30mg/kg.AtthisdoseinHCT116tumortissue,MLN8054hasbeenshowntoinhibitAuroraAautophosphorylation,andinduceanincreaseintheAuroraBsubstrate,pHisH3[2].PROTOCOLCellAssay[1]MLN8054isaddedtohumantumorcellsin2-foldserialdilutionstoachievefinalconcentrationsrangingfrom10to0.04mM.MLN8054ateachdilutionisaddedintriplicatewitheachreplicateonaseparateplate.CellstreatedwithDMSO(n=6wellsperplate;0.2%finalconcentration)servedastheuntreatedcontrol.ThecellsaretreatedwithMLN8054for96hat37°Cinahumidifiedcellculturechamber.CellviabilityineachcelllineismeasuredbyusingtheCellProliferationELISA,BrdUcolorimetrickit[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:NudemicebearingHCT-116tumorsaretreatedorallyonceperdayfor21consecutivedayswitheitherAdministration[1]vehiclecontrolorMLN8054atdosesof3,10,or30mg/kg.Tumorvolumesaremeasuredbyusingaverniercaliperandcalculated[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?SciTranslMed.2018Jul18;10(450).pii:eaaq1093.?CancerRes.2017Sep15;77(18):4785-4796.?PLoSBiol.2020Jun9;18(6):e3000288.?EMBORep.(2021)e51847.?ComputStructBiotechnolJ.2019Feb8;17:352-361.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ManfrediMG,etal.AntitumoractivityofMLN8054,anorallyactivesmall-moleculeinhibitorofAuroraAkinase.ProcNatlAcadSciUSA.2007Mar6;104(10):4106-11.[2].HuckJJ,etal.MLN8054,aninhibitorofAuroraAkinase,inducessenescenceinhumantumorcellsbothinvitroandinvivo.MolCancerRes.2010Mar;8(3):373-84