ZM-336372-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZM336372Cat.No.:HY-13343CASNo.:208260-29-1分⼦式:C₂₃H₂₃N₃O₃分⼦量:389.45作⽤靶点:Raf;Apoptosis作⽤通路:MAPK/ERKPathway;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(128.39mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5677mL12.8386mL25.6772mL5mM0.5135mL2.5677mL5.1354mL10mM0.2568mL1.2839mL2.5677mL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。-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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.42mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.42mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.42mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ZM336372⼀种有效的蛋⽩激酶c-Raf抑制剂。在含有0.1mMATP的情况下，IC50值为0.07μM。IC50&Targetc-Raf0.07μM(IC50,0.1mMATP)体外研究ZM336372isapotentinhibitorofhumanc-Raf.TheIC50valueis0.07μMinthestandardassay,whichcontains0.1mMATP.TheIC50,decreasesto0.01μMat0.025mMATPandincreasesto0.9μMat2.5mMATPindicatingthatZM336372isacompetitiveinhibitorwithrespecttoATP.ZM336372inhibitsc-RaftenfoldmorepotentlythanB-Raf[1].CellproliferationanalysisofZM336372.3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromidegrowthassayofH727andBONtreatedascontrol,DMSO,and100μMZM336372todays16and10,respectively.BothH727andBONcellproliferationisinhibitedinthepresenceofdrugcomparedwithcontrols.H727cellstreatedwithZM336372aregrowthsuppressed,whereascontroltreatmentshavesignificantlymoregrowthbyday6,continuingupto16days.AsimilarresponseisalsoseeninBONcellsasgrowthsuppressionoccurredasearlyasday4andwasmaintainedouttoday10[2].PROTOCOLCellAssay[2]ProliferationofH727andBONcellsaftertreatmentwithZM336372ismeasuredusinga3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide.Cellsaretrypsinizedandplatedintriplicateto24-wellplatesandallowedtoadhereovernight.Then,cellsaretreatedwitheither100μMZM336372orDMSO(2%)andincubated.Mediaarechangedevery2dayswithnewtreatment.Ateachtimepoint,cellgrowthratesareanalyzedaftertheadditionof3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromidereagenttotheculturedcells.Absorbanceisdeterminedusingspectrophotometeratawavelengthof540nm[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].Hall-JacksonCA,etal.ParadoxicalactivationofRafbyanovelRafinhibitor.ChemBiol.1999Aug;6(8):559-68.[2].VanGompelJJ,etal.ZM336372,aRaf-1activator,suppressesgrowthandneuroendocrinehormonelevelsincarcinoidtumorcells.MolCancerTher.2005Jun;4(6):910-7.McePdfHeightCaution:Producthasnotbeenfu