ProductDescription
OSI-906(Linsitinib)isanorally-available,ATP-competitive,imidazopyrazine-baseddualinhibitorofIGF-R1andIRwithIC50biochemicalpotencyof35nMand75nM,respectively.[1]InvitrocellassaysrevealthatOSI-906potentlyinhibitsIGF-1R,pERK1/2,andp-70S6KatIC50sof24,28,and60nM,respectively.InHT-29andColo205CRCcells,oSI-906fullyinhibitsbothIRandIGF-1Rphosphorylation,withantiproliferativeeffectsatEC50of210nMand320nM,respectively.
Oral,invivoefficacystudies(QDx12)ofOSI-906inaLISNxenograftmodelresultedinadose-dependenteffectontumorgrowthinhibitionwith100%TGIand55%regressionat75mg/kg,and60%TGIat25mg/kg.
Technicalinformation:
ChemicalFormula: | C26H23N5O | |
CAS#: | 867160-71-2 | |
MolecularWeight: | 421.49 | |
Purity: | >98% | |
Appearance: | Yellow | |
ChemicalName: | (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol | |
Solubility: | Upto100mMinDMSO | |
Synonyms: | OSI-906,OSI906,OSI906,Linsitinib |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | Mulvihilletal.,DiscoveryofOSI-906:aselectiveandorallyefficaciousdualinhibitoroftheIGF-1receptorandinsulinreceptor.FutureMed.Chem.2009,1(6),1153-1171.PubmedID:21425998 |
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