ProductDescription
LGK974isapotentandorallyactiveWntpathwayinhibitorwithanIC50<1nMintheWntsignalingassay[1].ItinhibitsacylationofWntproteinsbyPorcupine(Porcn).LGK974specificallyblockstheproliferationofpancreaticcancercellsthathaveup-regulatedWntsignalingcausedbycarryinginactivemutationsinaUbiquitinE3ligase,RNF43[2].
LGK974robustlysuppressedWntsignalinginvivoresultingintumorregressioninamurinebreastcancermodeldrivenbyMMTV-Wnt1,andshowedexcellentefficacyinxenograftmodelsofheadandnecksquamouscellcarcinomaandpancreaticcancer[3].CurrentlyLGK974isinthePhaseIstudytotreatpatientswithdifferenttypesofWntsignaling-drivencancers[4].
Technicalinformation:
| ChemicalFormula: | C23H20N6O | |
| CAS#: | 1243244-14-5 | |
| MolecularWeight: | 396.44 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 2-(2",3-dimethyl-[2,4"-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | NVP-LGK974,LGK974 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderorDMSOsolutionat-20oCdesiccated.
Reference:
| 1. | ShifengPan.DiscoveryofLGK974:AselectivePorcupineinhibitortargetingWntsignalingincancer.AACRAnnualMeeting2013. |
| 2. | JiangX,etal.InactivatingmutationsofRNF43conferWntdependencyinpancreaticductaladenocarcinoma.ProcNatlAcadSciUSA.2013;110(31):12649-54.PubmedID:23847203 |
| 3. | LiuJ,etal.TargetingWnt-drivencancerthroughtheinhibitionofPorcupinebyLGK974.ProcNatlAcadSciUSA.2013;110(50):20224-9PubmedID:24277854 |
| 4. | http://clinicaltrials.gov/show/NCT01351103 |
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