LCL-161isasecondmitochondria-derivedactivatorofcaspases(SMAC)mimeticthatbindstocIAP1andcIAP2(membersoftheinhibitorsofapoptosisfamilyofproteins,oftenupregulatedinmanycancers)andinitiatestheirdestruction.Thiscompoundexhibitsanticancerchemotherapeuticactivitybyinducingapoptosisininvitromodelsoflymphoidcancers.LCL-161alsoactivateshumanPXRandinducesactivityofCYP3A4/5.
| CasNo. | 1005342-46-0 |
|---|---|
| Purity | ≥99%,≥99%ee,de |
| Formula | C26H33FN4O3S |
| FormulaWt. | 500.63 |
| IUPACName | (2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide |
| Synonym | LCL161 |
| Solubility | InDMSO |
| Appearance | whitepowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | L1044InfoSheetPDF |
|---|
DhuriaS,EinolfH,MangoldJ,etal.Time-dependentinhibitionandinductionofhumancytochromeP4503A4/5byanoralIAPantagoNIST,LCL161,invitroandinvivoinhealthysubjects.JClinPharmacol.2013Jun;53(6):642-53.PMID:23585187.
HoughtonPJ,KangMH,ReynoldsCP,etal.Initialtesting(stage1)ofLCL161,aSMACmimetic,bythePediatricPreclinicalTestingProgram.PediatrBloodCancer.2012Apr;58(4):636-9.PMID:21681929.
