CanertinibisanirreversIBLeinhibitorofEGFR(HER2/ErbB).Thiscompoundiscurrentlyinclinicaltrialsasananticancerchemotherapeutic,displayingactivityagainstavarietyofcancers.Inacellularmodelofmelanoma,canertinibexhibitscytostaticactivity,stoppingcellgrowthintheG1phase,butnotinducingapoptosisexceptatveryhighconcentrations.Inarelatedanimalmodel,canertinibinhibitstumorgrowth.Separately,canertinibinhibitsAktandERK1/2incellslackingErbBreceptorsandinducescaspase-mediatedapoptosis.
| CasNo. | 289499-45-2 |
|---|---|
| Purity | ≥98% |
| Formula | C24H23ClFN5O3•2HCl |
| FormulaWt. | 558.86 |
| IUPACName | N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide;dihydrochloride |
| Synonym | CI1033 |
| Appearance | Paleyellowpowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | C0252InfoSheetPDF |
|---|---|
| Brochures | PI3K-Akt-mTORCPathwayBooklet |
Ras-Raf-MEK-ERKPathwayBooklet |
DjerfSeverinssonEA,TrinksC,GréenH,etal.Thepan-ErbBreceptortyrosinekinaseinhibitorcanertinibpromotesapoptosisofmalignantmelanomainvitroanddisplaysanti-tumoractivityinvivo.BiochemBiophysResCommun.2011Oct28;414(3):563-8.PMID:21982771.
TrinksC,SeverinssonEA,HolmlundB,etal.Thepan-ErbBtyrosinekinaseinhibitorcanertinibinducescaspase-mediatedcelldeathinhumanT-cellleukemia(Jurkat)cells.BiochemBiophysResCommun.2011Jul8;410(3):422-7.PMID:21669187.
ZinnerRG,NemunaitisJ,EisemanI,etal.PhaseIclinicalandpharmacodynamicevaluationoforalCI-1033inpatientswithrefractorycancer.ClinCancerRes.2007May15;13(10):3006-14.PMID:17505003.
