AZ13705339-hemihydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZ13705339hemihydrateCat.No.:HY-120940A分⼦式:C₃₃H₃₆FN₇O₃S.₁/₂H₂O分⼦量:638.77作⽤靶点:PAK作⽤通路:CellCycle/DNADamage;Cytoskeleton储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(156.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5655mL7.8275mL15.6551mL5mM0.3131mL1.5655mL3.1310mL10mM0.1566mL0.7828mL1.5655mL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。BIOLOGICALACTIVITY⽣物活性AZ13705339hemihydrate⼀种⾼效且具有选择性的PAK1抑制剂，对PAK1和pPAK1的IC50分别为0.33nM和59nM。AZ13705339hemihydrate对PAK1和PAK2具有结合亲和⼒，Kd分别为0.28nM和0.32nM。AZ13705339hemihydrate可⽤于癌症研究。IC50&TargetPAK2PAK1PAK1pPAK10.32nM(Kd)0.28nM(Kd)0.33nM(IC50)59nM(IC50)体外研究AZ13705339(1μM)hemihydrateinhibitsαIgM-controlledadhesionandnotPMA-inducedadhesionin1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemENamalwacells[2].AZ13705339(300nM,30min)preventsSiglec-8engagement-inducedeosinophildeath[3].体内研究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