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PotentALKinhibitor(IC50valuesare1.3,2.4,85.8,2,133and9,276nMforALK2,ALK1,ALK3,ALK4andALK5,respectively).ExhibitsselectivityforALK2overALK4andALK5incellularassays.InhibitsheterotopicossificationinamutantALK2mousemodeloffibrodysplasiaossificansprogressiva.AlsoexhibitsactivityagainstRIPK2,ABL1andPDGFR-β(IC50values<100nM).
SoldforresearchpurposesunderexclusiveagreementfromTheBrighamandWomen"sHospitalInc.USpatent14/776,302
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight406.48.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Mohedasetal(2013)DevelopmentofanALK2-biasedBMPtypeIreceptorkinaseinhibitor.ACSChem.Biol.81291PMID:23547776
Keywords:LDN212854,supplier,LDN212854,ALK,inhibitors,inhibits,potent,in,vivo,active,BMP1,ALK2,bone,morphogenetic,protein,type,I,BMP,and,Other,Activin,Receptors,BMP,and,Other,Activin,Receptors,TocrisBioscience
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