MedKooCat#:201436
Name:GPI-15427
CAS#:805242-85-7
ChemicalFormula:C20H20N4O2
ExactMass:348.15863
MolecularWeight:348.4
ElementalAnalysis:C,68.95;H,5.79;N,16.08;O,9.18
Synonym:GPI15427;GPI15427;GPI-15427.
IUPAC/ChemicalName:10-((4-methylpiperazin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one.
InChiKey:DZRLVSOGARUEGQ-UHFFFAOYSA-N
InChiCode:InChI=1S/C20H20N4O2/c1-23-7-9-24(10-8-23)12-13-5-6-16-15(11-13)19-18-14(20(25)22-21-19)3-2-4-17(18)26-16/h2-6,11H,7-10,12H2,1H3,(H,22,25)
SMILESCode:O=C1NN=C2C3=C1C=CC=C3OC4=C2C=C(CN5CCN(C)CC5)C=C4
TechnicalData
AdditionalInformation
GPI15427+radiationsignificantlyreducedtumorvolumecomparedtovehicletreatedmiceandmicetreatedwithGPI15427aloneormicetreatedwithradiationalone.Inconclusion,thesedataindicatethativadmiNISTrationofthePARPinhibitorGPI15427iswelltoleratedandinducessignificantenhancementofradiationanti-tumorefficacyagainsthumanheadandneckcancer.(source:http://aacrmeetingabstracts.org/cgi/content/abstract/2004/1/311-c).
References
1:KhanK,ArakiK,WangD,LiG,LiX,ZhangJ,XuW,HooverRK,LauterS,O'MalleyBJr,LapidusRG,LiD.Headandneckcancerradiosensitizationbythenovelpoly(ADP-ribose)polymeraseinhibitorGPI-15427.HeadNeck.2010Mar;32(3):381-91.doi:10.1002/hed.21195.PubMedPMID:19672867.
2:DiPaolaR,MazzonE,XuW,GenoveseT,FerrrarisD,Muià C,CrisafulliC,ZhangJ,CuzzocreaS.TreatmentwithPARP-1inhibitors,GPI15427orGPI16539,amelioratesintestinaldamageinratmodelsofcolitisandshock.EurJPharmacol.2005Dec19;527(1-3):163-71.Epub2005Nov28.PubMedPMID:16310767.
3:TentoriL,LeonettiC,ScarsellaM,VergatiM,XuW,CalvinD,MorganL,TangZ,WoznizkK,AlemuC,HooverR,LapidusR,ZhangJ,GrazianiG.BraindistributionandefficacyaschemosensitizerofanoralformulationofPARP-1inhibitorGPI15427inexperimentalmodelsofCNStumors.IntJOncol.2005Feb;26(2):415-22.PubMedPMID:15645126.
4:TentoriL,LeonettiC,ScarsellaM,D'AmatiG,VergatiM,PortarenaI,XuW,KalishV,ZupiG,ZhangJ,GrazianiG.SystemicadministrationofGPI15427,anovelpoly(ADP-ribose)polymerase-1inhibitor,increasestheantitumoractivityoftemozolomideagainstintracranialmelanoma,glioma,lymphoma.ClinCancerRes.2003Nov1;9(14):5370-9.PubMedPMID:14614022.
