Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAZ13705339hemihydrateCat.No.:HY-120940A分?式:C??H??FN?O?S.?/?H?O分?量:638.77作?靶點(diǎn):PAK作?通路:CellCycle/DNADamage;Cytoskeleton儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(156.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5655mL7.8275mL15.6551mL5mM0.3131mL1.5655mL3.1310mL10mM0.1566mL0.7828mL1.5655mL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。-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AZ13705339hemihydrate?種?效且具有選擇性的PAK1抑制劑，對PAK1和pPAK1的IC50分別為0.33nM和59nM。AZ13705339hemihydrate對PAK1和PAK2具有結(jié)合親和?，Kd分別為0.28nM和0.32nM。AZ13705339hemihydrate可?于癌癥研究。IC50&TargetPAK2PAK1PAK1pPAK10.32nM(Kd)0.28nM(Kd)0.33nM(IC50)59nM(IC50)體外研究AZ13705339(1μM)hemihydrateinhibitsαIgM-controlledadhesionandnotPMA-inducedadhesionin1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemENamalwacells[2].AZ13705339(300nM,30min)preventsSiglec-8engagement-inducedeosinophildeath[3].體內(nèi)研究AZ13705339hemihydrate(100mg/kg,P.O.)hasmoderateclearanceandoralCmaxof7.7μMinrats[1].REFERENCES[1].McCoullW,etal.OptimizationofHighlyKinaseSelectiveBis-anilinoPyrimidinePAK1Inhibitors.ACSMedChemLett.2016;7(12):1118-1123.Published2016Sep14.[2].MartinFMdeRooij,etal.Aloss-of-adhesionCRISPR-Cas9screeningplatformtoidentifycelladhesion-regulatoryproteinsandsignalingpathways.NatCommun.2022Apr19;13(1):2136.[3].DanielaJCarroll,etal.Siglec-8SignalsThroughaNon-CanonicalPathwaytoCauseHumanEosinophilDeathInVitro.FrontImmunol.2021Oct11;12:737988.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-379