ZM-336372-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZM336372Cat.No.:HY-13343CASNo.:208260-29-1分?式:C??H??N?O?分?量:389.45作?靶點(diǎn):Raf;Apoptosis作?通路:MAPK/ERKPathway;Apoptosis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:50mg/mL(128.39mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5677mL12.8386mL25.6772mL5mM0.5135mL2.5677mL5.1354mL10mM0.2568mL1.2839mL2.5677mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.42mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.42mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.42mM);ClearsolutionBIOLOGICALACTIVITY?物活性ZM336372?種有效的蛋?激酶c-Raf抑制劑。在含有0.1mMATP的情況下，IC50值為0.07μM。IC50&Targetc-Raf0.07μM(IC50,0.1mMATP)體外研究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