CEP-28122-mesylate-salt-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECEP-28122mesylatesaltCat.No.:HY-18030A分⼦式:C₂₉H₃₉ClN₆O₆S分⼦量:635.17作⽤靶点:Anaplasticlymphomakinase(ALK)作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥6.4mg/mL(10.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5744mL7.8719mL15.7438mL5mM0.3149mL1.5744mL3.1488mL10mM0.1574mL0.7872mL1.5744mL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(sealedstorage,awayfrommoisture)。-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。BIOLOGICALACTIVITY⽣物活性CEP-28122mesylatesalt⼀种⼆氨嘧啶衍⽣物，⼀种⾼度有效的选择性且具有⼝服活性的ALK抑制剂，对重组ALK激酶活性的IC50为1.9nM。CEP-28122在⼈类癌症的ALK阳性实验模型中具有抗肿瘤活性。CEP-28122具有良好的药效药代活性。体外研究CEP-28122mesylatesalt(3-3000nM;48hours)treatmentleadstoconcentration-dependentgrowthinhibitionofKarpas-299andSup-M2cellsinculture,associateswithconcentration-relatedcaspase3/7activation[1].CEP-28122mesylatesalt(30-1000nM;2hours)treatmentleadstosubstantialsuppressionof1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师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.体内研究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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidate