MolecularWeight: | 396.44 |
Formula: | C23H20N6O |
Purity: | ≥98% |
CAS#: | 1243244-14-5 |
Solubility: | DMSOupto100mM |
ChemicalName: | 2-(2",3-dimethyl-[2,4"-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide |
Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
LGK974isahighlypotent,selectiveandorallybioavailablePorcupineinhibitor(WntsignalingantagoNIST)withanIC50~0.4nM.LGK974potentlyinhibitsWntsignalinginvitroandinvivo,includingreductionoftheWnt-dependentLRP6phosphorylationandtheexpressionofWnttargetgenes,suchasAXIN2.LGK974ispotentandefficaciousinmultipletumormodelsatwell-tolerateddosesinvivo,includingmurineandratmechanisticbreastcancermodelsdrivenbyMMTV–Wnt1andahumanheadandnecksquamouscellcarcinomamodel(HN30).Wealsoshowthatheadandneckcancercelllineswithloss-of-functionmutationsintheNotchsignalingpathwayhaveahighresponseratetoLGK974.CurrentlyLGK974isinthePhaseIstudytotreatcancersthataredrivenbytheWntpathwayinaWntligand-dependentmanner.
HowtoUse:
- Invitro:LGK974wassuggestedtobeusedat0.1µMfinalconcentrationinvitrotocompletelyblockWntproteinsecretion.
- Invivo:LGK974wasusedtodosemiceorallyat0.1-10mg/kgonceortwiceperdaytoachievegoodefficacyinxenograftmodels.
Reference:
- 1.LiuJ,etal.TargetingWnt-drivencancerthroughtheinhibitionofPorcupinebyLGK974.(2013)ProcNatlAcadSciUSA.110(50):20224-9.
- 2.JiangX,etal.InactivatingmutationsofRNF43conferWntdependencyinpancreaticductaladenocarcinoma.(2013)ProcNatlAcadSciUSA.110(31):12649-54.
- 3.ShifengPan.DiscoveryofLGK974:AselectivePorcupineinhibitortargetingWntsignalingincancer.AACRAnnualMeeting2013.
- LGK974_spec.pdf
- LGK974_MSDS.pdf
Productsareforresearchuseonly.Notforhumanuse.
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