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| 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.
Xcess生物科学公司(XcessBio)成立于2008年,由一群顶尖的科学家来自学术界和制药/生物技术产业具有较强的专业知识在药物化学、生物化学、分子和细胞生物学。
