CEP-28122-mesylate-salt-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECEP-28122mesylatesaltCat.No.:HY-18030A分?式:C??H??ClN?O?S分?量:635.17作?靶點(diǎn):Anaplasticlymphomakinase(ALK)作?通路:ProteinTyrosineKinase/RTK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(shí)驗DMSO:≥6.4mg/mL(10.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5744mL7.8719mL15.7438mL5mM0.3149mL1.5744mL3.1488mL10mM0.1574mL0.7872mL1.5744mL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?。BIOLOGICALACTIVITY?物活性CEP-28122mesylatesalt?種?氨嘧啶衍?物，?種?度有效的選擇性且具有?服活性的ALK抑制劑，對重組ALK激酶活性的IC50為1.9nM。CEP-28122在?類癌癥的ALK陽性實(shí)驗?zāi)Ｐ椭芯哂锌鼓[瘤活性。CEP-28122具有良好的藥效藥代活性。體外研究CEP-28122mesylatesalt(3-3000nM;48hours)treatmentleadstoconcentration-dependentgrowthinhibitionofKarpas-299andSup-M2cellsinculture,associateswithconcentration-relatedcaspase3/7activation[1].CEP-28122mesylatesalt(30-1000nM;2hours)treatmentleadstosubstantialsuppressionof1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEphosphorylationofputativedownstreameffectorsofALKinSup-M2cells,indicatingthatthedownstreamsignalingpathwaysaremediatedbyindividualALKfusionprotein[1].CellCytotoxicityAssay[1]CellLine:Karpas-299,Sup-M2,ToledoandHuT-102cellsConcentration:10nM,100nM,1000nM,10000nMIncubationTime:48hoursResult:Treatmentledtoconcentration-dependentgrowthinhibitionofKarpas-299andSup-M2cellsinculture.WesternBlotAnalysis[1]CellLine:Sup-M2cellsConcentration:30nM,100nM,300nM,1000nMIncubationTime:2hoursResult:ResultedinsubstantialsuppressionofphosphorylationofputativedownstreameffectorsofALK,includingStat-3,Akt,andERK1/2inSup-M2cells.體內(nèi)研究CEP-28122mesylatesalt(3-30mg/kg;oralgavage;twiceaday;12days)producesdose-dependentantitumoractivityinSup-M2subcutaneoustumorxenograftsinSCIDmice.Incontrast,CEP-28122hasnoantitumoractivityinnu/numicebearingHCT116,suggestingthattheantitumoractivityofCEP-28122inNPM-ALK–positiveSup-M2tumormodelsisduetosustainedNPM-ALKinhibitionintumors[1].AnimalModel:FemaleSCIDmicebearingSup-M2subcutaneoustumorxenograftsandnu/numicebearingHCT116aged6-8weekold[1]Dosage:3mg/kg,10mg/kgand30mg/kgAdministration:oralgavage;twiceaday;12daysResult:CEP-28122produceddose-dependentantitumoractivityinSup-M2subcutaneoustumorxenograftsinSCIDmice.Incontrast,CEP-28122hadnoantitumoractivityinnu/numicebearingHCT116.REFERENCES[1].MangengCheng,etal.CEP-28122,ahighlypotentandselectiveorallyactiveinhibitorofanaplasticlymphomakinasewithantitumoractivityinexperimentalmodelsofhumancancers.MolCancerTher.2012Mar;11(3):670-9.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidate