NVP-TAE684isaninhibitorofanaplasticlymphomakinase(ALK),c-Fes,andLRRK2thatexhibitsanticancerchemotherapeuticactivity.NVP-TAE684inducesapoptosisinandinhibitsgrowthofdiffuselargeB-celllymphomacells;inanimalmodels,itinducestumorregression.NVP-TAE684alsoinducescellcyclearrestandapoptosisinanimalmodelsofanaplasticlarge-celllymphoma,preventinglymphomagenesisandinducingregression.
| CasNo. | 761439-42-3 |
|---|---|
| Purity | ≥98% |
| Formula | C30H40ClN7O3S |
| FormulaWt. | 614.21 |
| IUPACName | 5-Chloro-N4-[2-(isopropylsulfonyl)phenyl]-N2-{2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl}-2,4-pyrimidinediamine |
| Synonym | TAE684 |
| Appearance | Yellowtopaleyellowpowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | N8760InfoSheetPDF |
|---|
HellwigS,MiduturuCV,KandaS,etal.Small-moleculeinhibitorsofthec-Fesprotein-tyrosinekinase.ChemBiol.2012Apr20;19(4):529-40.PMID:22520759.
ZhangJ,DengX,ChoiHG,etal.CharacterizationofTAE684asapotentLRRK2kinaseinhibitor.BioorgMedChemLett.2012Mar1;22(5):1864-9.PMID:22335897.
CerchiettiL,Damm-WelkC,VaterI,etal.Inhibitionofanaplasticlymphomakinase(ALK)activityprovidesatherapeuticapproachforCLTC-ALK-positivehumandiffuselargeBcelllymphomas.PLoSOne.2011Apr8;6(4):e18436.PMID:21494621.
GalkinAV,MelnickJS,KimS,etal.IdentificationofNVP-TAE684,apotent,selective,andefficaciousinhibitorofNPM-ALK.ProcNatlAcadSciUSA.2007Jan2;104(1):270-5.Erratumin:ProcNatlAcadSciUSA.2007Feb6;104(6):2025.PMID:17185414.
