Description
CAL101isaninhibitorofp110δPI3Kthatisclinicallyusedtotreatleukemiassuchasmantlecelllymphomaandchroniclymphocyticleukemia(CLL).CAL101exhibitsanticancerchemotherapeuticandimmunosuppressiveactivities.Inmantlecelllymphomacells,CAL101inducesG1phasecellcyclearrestandapoptosis.Innon-HodgkinlymphomaandCLLcells,CAL101inhibitsdownstreamphosphorylationofAktandinducesapoptosis.Additionally,thiscompoundinhibitscellchemotaxis,decreaseschemokineproduction,inhibitsmigration,andpreventsERK-andAkt-dependentB-cellreceptorsignalinginCLLcells.
References
SanfordDS,WierdaWG,BurgerJA,etal.ThreeNewlyApprovedDrugsforChronicLymphocyticLeukemia:IncorporatingIbrutinib,Idelalisib,andObinutuzumabintoClinicalPractice.ClinLymphomaMyelomaLeuk.2015Feb19.[Epubaheadofprint].PMID:25817936.
ChironD,MartinP,DiLibertoM,etal.InductionofprolongedearlyG1arrestbyCDK4/CDK6inhibitionreprogramslymphomacellsfordurablePI3KδinhibitionthroughPIK3IP1.CellCycle.2013Jun15;12(12):1892-900.PMID:23676220.
MeadowsSA,VegaF,KashishianA,JohnsonD,etal.PI3Kδinhibitor,GS-1101(CAL-101),attenuatespathwaysignaling,inducesapoptosis,andovercomessignalsfromthemicroenvironmentincellularmodelsofHodgkinlymphoma.Blood.2012Feb23;119(8):1897-900.PMID:22210877.
HoellenriegelJ,MeadowsSA,SivinaM,etal.Thephosphoinositide3"-kinasedeltainhibitor,CAL-101,inhibitsB-cellreceptorsignalingandchemokinenetworksinchroniclymphocyticleukemia.Blood.2011Sep29;118(13):3603-12.PMID:21803855.
