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MedKoo Biosciences/GDC0941 (Pictilisib)/201395/10mg

Pictilisib,alsoknownasPictrelisib,GDC-0941,RG7321andGNE0941,isanorallybioavailable,andisapotentsmall-moleculethieno[3,2-d]pyrimidineinhibitoroftheclassIphosphatidylinositol3kinase(PI3K)isoformsp100alphaandp100deltawithpotentialantineoplasticactivity.PI3KinhibitorGDC-0941selectivelybindstoPI3KisoformsinanATP-competitivemanner,inhibitingtheproductionofthesecondarymessengerphosphatidylinositol-3,4,5-trisphosphate(PIP3)andactivationofthePI3K/Aktsignalingpathway;inhibitionoftumorcellgrowth,motilityandsurvivalinsusceptibletumorcellpopulationsmayresult.

MedKooCat#:201395
Name:GDC-0941(Pictilisib)
CAS#:957054-30-7(freebase);957054-33-0(mesylate).
ChemicalFormula:C23H27N7O3S2
ExactMass:513.16168
MolecularWeight:513.63
ElementalAnalysis:C,53.78;H,5.30;N,19.09;O,9.34;S,12.49


Synonym:GDC-0941;GDC0941;GDC0941;RG7321;RG-7321;RG7321;GNE0941;GNE-0941;GNE0941;Pictrelisib;Pictilisib

IUPAC/ChemicalName:4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine

InChiKey:LHNIIDJUOCFXAP-UHFFFAOYSA-N

InChiCode:InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)

SMILESCode:O=S(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)(C)=O


TechnicalData

Appearance:
Whitetooff-whitesolidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:
ViewCoA:currentbatch,lot#BBC50329

QCData:
ViewQCdata:currentbatch,lot#BBC50329

SafetyDataSheet(MSDS):
ViewMaterialSafetyDataSheet(MSDS)

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:
Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:
SolubleinDMSO,notinwater

ShelfLife:
>2yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:
0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:
293490


References

1:EhrhardtM,CraveiroRB,HolstMI,PietschT,DillooD.ThePI3KinhibitorGDC-0941displayspromisinginvitroandinvivoefficacyfortargetedmedulloblastomatherapy.Oncotarget.2015Jan20;6(2):802-13.PubMedPMID:25596739.

2:SarkerD,AngJE,BairdR,KristeleitR,ShahK,MorenoV,ClarkePA,RaynaudFI,LevyG,WareJA,MazinaK,LinR,WuJ,FredricksonJ,SpoerkeJM,LacknerMR,YanY,FriedmanLS,KayeSB,DerynckMK,WorkmanP,deBonoJS.First-in-humanphaseIstudyofpictilisib(GDC-0941),apotentpan-classIphosphatidylinositol-3-kinase(PI3K)inhibitor,inpatientswithadvancedsolidtumors.ClinCancerRes.2015Jan1;21(1):77-86.doi:10.1158/1078-0432.CCR-14-0947.Epub2014Nov4.PubMedPMID:25370471;PubMedCentralPMCID:PMC4287394.

3:SalphatiL,Shahidi-LathamS,QuiasonC,BarckK,NishimuraM,AlickeB,PangJ,CaranoRA,OliveroAG,PhillipsHS.Distributionofthephosphatidylinositol3-kinaseinhibitorsPictilisib(GDC-0941)andGNE-317inU87andGS2intracranialglioblastomamodels-assessmentbymatrix-assistedlaserdesorptionionizationimaging.DrugMetabDispos.2014Jul;42(7):1110-6.doi:10.1124/dmd.114.057513.Epub2014Apr22.PubMedPMID:24754926.

4:ZhengJ,WangH,YaoJ,ZouX.MoreantitumorefficacyofthePI3KinhibitorGDC-0941inbreastcancerwithPIK3CAmutationorHER2amplificationstatusinvitro.Pharmazie.2014Jan;69(1):38-42.PubMedPMID:24601221.

5:WareJA,DalzielG,JinJY,PellettJD,SmelickGS,WestDA,SalphatiL,DingX,SuttonR,FridylandJ,DresserMJ,MorrissonG,HoldenSN.ImpactoffoodandtheprotonpumpinhibitorrabeprazoleonthepharmacokineticsofGDC-0941inhealthyvolunteers:benchtobedsideinvestigationofpH-dependentsolubility.MolPharm.2013Nov4;10(11):4074-81.doi:10.1021/mp4005595.Epub2013Oct24.PubMedPMID:24099279.

6:PangJ,DalzielG,DeanB,WareJA,SalphatiL.PharmacokineticsandabsorptionoftheanticanceragentsdasatinibandGDC-0941undervariousgastricconditionsindogs--reversingtheeffectofelevatedgastricpHwithbetaineHCl.MolPharm.2013Nov4;10(11):4024-31.doi:10.1021/mp400356m.Epub2013Sep11.PubMedPMID:23980865.

7:JinL,TabeY,KojimaK,ShikamiM,BenitoJ,RuvoloV,WangRY,McQueenT,CiureaSO,MiidaT,AndreeffM,KonoplevaM.PI3KinhibitorGDC-0941enhancesapoptoticeffectsofBH-3mimeticABT-737inAMLcellsinthehypoxicbonemarrowmicroenvironment.JMolMed(Berl).2013Dec;91(12):1383-97.doi:10.1007/s00109-013-1076-3.Epub2013Aug18.PubMedPMID:23955073;PubMedCentralPMCID:PMC3834093.

8:CawthorneC,BurrowsN,GielingRG,MorrowCJ,ForsterD,GregoryJ,RadigoisM,SmigovaA,BaburM,SimpsonK,HodgkinsonC,BrownG,McMahonA,DiveC,HiscockD,WilsonI,WilliamsKJ.[18F]-FLTpositronemissiontomographycanbeusedtoimagetheresponseofsensitivetumorstoPI3-kinaseinhibitionwiththenovelagentGDC-0941.MolCancerTher.2013May;12(5):819-28.doi:10.1158/1535-7163.MCT-12-0905.Epub2013Feb20.PubMedPMID:23427298;PubMedCentralPMCID:PMC3670082.

9:MunugalavadlaV,MariathasanS,SlagaD,DuC,BerryL,DelRosarioG,YanY,BoeM,SunL,FriedmanLS,ChesiM,LeifBergsagelP,EbensA.ThePI3KinhibitorGDC-0941combineswithexistingclinicalregimensforsuperioractivityinmultiplemyeloma.Oncogene.2014Jan16;33(3):316-25.doi:10.1038/onc.2012.594.Epub2013Jan14.PubMedPMID:23318440.

10:FlorisG,WozniakA,SciotR,LiH,FriedmanL,VanLooyT,WellensJ,VermaelenP,DerooseCM,FletcherJA,Debiec-RychterM,SchöffskiP.ApotentcombinationofthenovelPI3KInhibitor,GDC-0941,withimatinibingastrointestinalstromaltumorxenografts:long-lastingresponsesaftertreatmentwithdrawal.ClinCancerRes.2013Feb1;19(3):620-30.doi:10.1158/1078-0432.CCR-12-2853.Epub2012Dec11.PubMedPMID:23231951.


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