BYL-719isanATP-competitiveoralPI3Kinhibitorselectiveforthep110αisoformthatisactivatedbyamutantPIK3CAgeneinHER2+breastcancersandgastriccancers.BYL-719exhibitsanticancerchemotherapeuticactivityandinhibitsproliferationinavarietyofcelllines.IGF1andneuregulin1activatemTOR,adownstreamtargetofPI3KthatmediatesresistancetoBYL-719insomeinvitrocancermodels.Thiscompoundalsodecreasesinvasionandepithelial-to-mesenchymaltransition(EMT)incellularandanimalmodelsofsquamouscelllungcancer.
| CasNo. | 1217486-61-7 |
|---|---|
| Purity | ≥99%,≥99%ee |
| Formula | C19H22F3N5O2S |
| FormulaWt. | 441.47 |
| IUPACName | (2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide |
| Synonym | Alpelisib,NVP-BYL719,BYL-719 |
| Solubility | InDMSO |
| Appearance | WhiteCrystalPowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | B9700InfoSheetPDF |
|---|
BonelliMA,CavazzoniA,SaccaniF,etal.InhibitionofPI3Kpathwayreducesinvasivenessandepithelial-to-mesenchymaltransitioninsquamouslungcancercelllinesharboringPIK3CAgenealterations.MolCancerTher.2015May26.[Epubaheadofprint].PMID:26013318.
ElkabetsM,VoraS,JuricD,etal.mTORC1InhibitionIsRequiredforSensitivitytoPI3Kp110αInhibitorsinPIK3CA-MutantBreastCancer.SciTranslMed.2013Jul31;5(196):196ra99.PMID:23903756.
Abstract:Juric.BYL719,anextgenerationPI3Kalphaspecificinhibitor:Preliminarysafety,PK,andefficacyresultsfromthefirst-in-humanstudy.AmericanAssociationforCancerResearch.2012.
