NeratinibisanirreversIBLeEGFRinhibitorthatdisplaysanticancerchemotherapeuticbenefitinthetreatmentofHER2positivebreastcancersandnon-smallcelllungcancer(NSCLC).Neratinibpreventsligand-inducedreceptordimerizationbytargetingacysteineresidueintheATPbindingpocketofthereceptor.Inpre-clinicalmodels,thiscompoundinducescellcyclearrestanddecreasescellproliferation.
| CasNo. | 698387-09-6 |
|---|---|
| Purity | ≥98% |
| Formula | C30H29ClN6O3 |
| FormulaWt. | 557.04 |
| ChemicalName | (2E)-N-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| IUPACName | (E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| Synonym | HKI-272,WAY-179272 |
| Appearance | Offwhitetoslightyellowpowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| MSDS | N1868MSDSPDF |
|---|---|
| InfoSheet | N1868InfoSheetPDF |
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Sánchez-MartínM,PandiellaA.DifferentialactionofsmallmoleculeHERkinaseinhibitorsonreceptorheterodimerization:therapeuticimplications.IntJCancer.2012Jul1;131(1):244-52.PMID:21826647.
WongKK,FracassoPM,BukowskiRM,etal.AphaseIstudywithneratinib(HKI-272),anirreversiblepanErbBreceptortyrosinekinaseinhibitor,inpatientswithsolidtumors.ClinCancerRes.2009Apr1;15(7):2552-8.PMID:19318484.
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