PelitinibisanirreversIBLeEFGRinhibitorthatexhibitsanticancerchemotherapeuticbenefitinthetreatmentofnon-smallcelllungcancer(NSCLC)andothersolidtumorcancers.Invitro,pelitinibinhibitsNF-κB,inhibitingtranscriptionofTERTandtelomeraseactivity.PelitinibalsodecreasesphosphorylationofAktandERKandinducescellcyclearrestinvitro.
| CasNo. | 257933-82-7 |
|---|---|
| Purity | ≥98% |
| Formula | C24H23ClFN5O2 |
| FormulaWt. | 467.92 |
| ChemicalName | (E)-N-(4-((3-chloro-4-fluorophenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide |
| IUPACName | (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| Synonym | EKB-569 |
| MeltingPoint | 188-190°C(lit.) |
| Solubility | Insolubleinwater.SoulbleinDMSO(≥13mg/mL). |
| Appearance | WhitePowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| MSDS | P1845MSDSPDF |
|---|---|
| InfoSheet | P1845InfoSheetPDF |
AravindanN,AravindanS,HermanTS,etal.EGFRtyrosinekinaseinhibitorpelitinibregulatesrADIation-inducedp65-dependenttelomeraseactivationinsquamouscellcarcinoma.RadiatRes.2013Mar;179(3):304-12.PMID:23379415.
KimH,LimHY.NovelEGFR-TKinhibitorEKB-569inhibitshepatocellularcarcinomacellproliferationbyAKTandMAPKpathways.JKoreanMedSci.2011Dec;26(12):1563-8.PMID:22147992.
YoshimuraN,KudohS,KimuraT,etal.EKB-569,anewirreversibleepidermalgrowthfactorreceptortyrosinekinaseinhibitor,withclinicalactivityinpatientswithnon-smallcelllungcancerwithacquiredresistancetogefitinib.LungCancer.2006Mar;51(3):363-8.PMID:16364494.
