MedKoo Biosciences/PCI24781 (Abexinostat)/202170/25mg

Synonym:CRA-024781;CRA024781;CRA024781;PCI24781;PCI-24781;PCI24781;Abexinostat.

IUPAC/ChemicalName:3-(dimethylaminomethyl)-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide

InChiKey:MAUCONCHVWBMHK-UHFFFAOYSA-N

InChiCode:InChI=1S/C21H23N3O5/c1-24(2)13-17-16-5-3-4-6-18(16)29-19(17)21(26)22-11-12-28-15-9-7-14(8-10-15)20(25)23-27/h4-10,27H,11-13H2,1-2H3,(H,22,26)(H,23,25)

SMILESCode:O=C(C(O1)=C(CN(C)C)C2=C1C=CC=C2)NCCOC3=CC=C(C(NO)=O)C=C3

TechnicalData

AdditionalInformation

References

1:Correction:CombiningPCI-24781,aNovelHistoneDeacetylaseInhibitor,withChemotherapyfortheTreatmentofSoftTissueSarcoma.ClinCancerRes.2015Apr1;21(7):1774-5.doi:10.1158/1078-0432.CCR-15-0351.PubMedPMID:25833311.

2:ShollerGS,CurrierEA,DuttaA,SlavikMA,IllenyeSA,MendoncaMC,DragonJ,RobertsSS,BondJP.PCI-24781(abexinostat),anovelhistonedeacetylaseinhibitor,inducesreactiveoxygenspecies-dependentapoptosisandissynergisticwithbortezomibinneuroblastoma.JCancerTherRes.2013Dec28;2:21.PubMedPMID:25520806;PubMedCentralPMCID:PMC4266584.

3:ZhangW,LvS,LiuJ,ZangZ,YinJ,AnN,YangH,SongY.PCI-24781down-regulatesEZH2expressionandthenpromotesgliomaapoptosisbysuppressingthePIK3K/Akt/mTORpathway.GenetMolBiol.2014Oct;37(4):716-24.doi:10.1590/S1415-47572014005000011.Epub2014Oct21.PubMedPMID:25505847;PubMedCentralPMCID:PMC4261972.

4:HeWL,LiYH,HouWJ,KeZF,ChenXL,LuLY,CaiSR,SongW,ZhangCH,HeYL.RAD51potentiatessynergisticeffectsofchemotherapywithPCI-24781andcis-diamminedichloroplatinumongastriccancer.WorldJGastroenterol.2014Aug7;20(29):10094-107.doi:10.3748/wjg.v20.i29.10094.PubMedPMID:25110436;PubMedCentralPMCID:PMC4123338.

5:ZhanQ,TsaiS,LuY,WangC,KwanY,NgaiS.RuvBL2isinvolvedinhistonedeacetylaseinhibitorPCI-24781-inducedcelldeathinSK-N-DZneuroblastomacells.PLoSOne.2013Aug16;8(8):e71663.doi:10.1371/journal.pone.0071663.eCollection2013.PubMedPMID:23977108;PubMedCentralPMCID:PMC3745445.

6:FouliardS,RobertR,Jacquet-BescondA,duRieuQC,BalasubramanianS,LouryD,LoriotY,HollebecqueA,KloosI,SoriaJC,ChenelM,DepilS.Pharmacokinetic/pharmacodynamicmodelling-basedoptimisationofadmiNISTrationscheduleforthehistonedeacetylaseinhibitorabexinostat(S78454/PCI-24781)inphaseI.EurJCancer.2013Sep;49(13):2791-7.doi:10.1016/j.ejca.2013.05.009.Epub2013Jun18.PubMedPMID:23790467.

7:ChalretduRieuQ,FouliardS,Jacquet-BescondA,RobertR,KloosI,DepilS,ChatelutE,ChenelM.Applicationofhematologicaltoxicitymodelinginclinicaldevelopmentofabexinostat(S-78454,PCI-24781),anewhistonedeacetylaseinhibitor.PharmRes.2013Oct;30(10):2640-53.doi:10.1007/s11095-013-1089-1.Epub2013Jun5.PubMedPMID:23737346.

8:KitamuraT,ConnollyK,RuffinoL,AjikiT,LueckgenA,DiGiovanniJ,KiguchiK.ThetherapeuticeffectofhistonedeacetylaseinhibitorPCI-24781ongallbladdercarcinomainBK5.erbB2mice.JHepatol.2012Jul;57(1):84-91.doi:10.1016/j.jhep.2012.01.018.Epub2012Feb9.PubMedPMID:22326466;PubMedCentralPMCID:PMC3378818.

9:YangC,ChoyE,HornicekFJ,WoodKB,SchwabJH,LiuX,MankinH,DuanZ.HistonedeacetylaseinhibitorPCI-24781enhanceschemotherapy-inducedapoptosisinmultidrug-resistantsarcomacelllines.AnticancerRes.2011Apr;31(4):1115-23.PubMedPMID:21508354;PubMedCentralPMCID:PMC3744220.

10:YangC,ChoyE,HornicekFJ,WoodKB,SchwabJH,LiuX,MankinH,DuanZ.Histonedeacetylaseinhibitor(HDACI)PCI-24781potentiatescytotoxiceffectsofdoxorubicininbonesarcomacells.CancerChemotherPharmacol.2011Feb;67(2):439-46.doi:10.1007/s00280-010-1344-7.Epub2010May12.PubMedPMID:20461381.