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MedKoo Biosciences/PRT-060318/406271/500mg

PRT-060318,alsoknownasPRT318orP142–76,isanovelselectiveinhibitorofthetyrosinekinaseSyk,asanapproachtoHITtreatment.PRT318completelyinhibitedHITimmunecomplex-inducedaggregationofbothhumanandtransgenicHITmouseplatelets.TransgenicHITmodelmiceweretreatedwithKKO,amousemonoclonalHIT-likeantibody,andheparin.TheexperimentalgroupreceivedorallydosedPRT318,whereasthecontrolgroupreceivedvehicle.NADIrplateletcountsofPRT318-treatedmiceweresignificantlyhigherthanthoseofcontrolmice.Whenexaminedwithanovelthrombosisvisualizationtechnique,micetreatedwithPRT318hadsignificantlyreducedthrombosis.

MedKooCat#:406271
Name:PRT-060318
CAS#:1194961-19-7
ChemicalFormula:C18H24N6O
ExactMass:340.20116
MolecularWeight:340.42
ElementalAnalysis:C,63.51;H,7.11;N,24.69;O,4.70


Synonym:PRT060318;PRT060318;PRT-060318;PRT318;PRT-318;PRT318;P14-276.

IUPAC/ChemicalName:2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide

InChiKey:NZNTWOVDIXCHHS-LSDHHAIUSA-N

InChiCode:InChI=1S/C18H24N6O/c1-11-5-4-6-12(9-11)22-17-13(16(20)25)10-21-18(24-17)23-15-8-3-2-7-14(15)19/h4-6,9-10,14-15H,2-3,7-8,19H2,1H3,(H2,20,25)(H2,21,22,23,24)/t14-,15+/m0/s1

SMILESCode:O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

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

Solubility:
solubleinDMSO,notsolubleinwater.

ShelfLife:
>5yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

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

HarmonizedSystemCode:
293490


AdditionalInformation

  
 
 
 


References

1:NanìS,FumagalliL,SinhaU,KamenL,ScapiniP,BertonG.SrcfamilykinasesandSykarerequiredforneutrophilextracellulartrapformationinresponsetoβ-glucanparticles.JInnateImmun.2015;7(1):59-73.doi:10.1159/000365249.Epub2014Sep24.PubMedPMID:25277753.

2:ChengS,GuoA,LuP,MaJ,ColemanM,WangYL.FunctionalcharacterizationofBTK(C481S)mutationthatconfersibrutinibresistance:explorationofalternativekinaseinhibitors.Leukemia.2015Apr;29(4):895-900.doi:10.1038/leu.2014.263.Epub2014Sep5.PubMedPMID:25189416.

3:HoellenriegelJ,CoffeyGP,SinhaU,PandeyA,SivinaM,FerrajoliA,RavandiF,WierdaWG,O'BrienS,KeatingMJ,BurgerJA.Selective,novelspleentyrosinekinase(Syk)inhibitorssuppresschroniclymphocyticleukemiaB-cellactivationandmigration.Leukemia.2012Jul;26(7):1576-83.doi:10.1038/leu.2012.24.Epub2012Feb7.PubMedPMID:22362000.

4:AndreP,MorookaT,SimD,AbeK,LowellC,NandaN,DelaneyS,SiuG,YanY,HollenbachS,PandeyA,GaoH,WangY,NakajimaK,ParikhSA,ShiC,PhillipsD,OwenW,SinhaU,SimonDI.CriticalroleforSykinresponsestovascularinjury.Blood.2011Nov3;118(18):5000-10.doi:10.1182/blood-2011-06-360743.Epub2011Aug31.PubMedPMID:21881044;PubMedCentralPMCID:PMC3208305.

5:ReillyMP,SinhaU,AndréP,TaylorSM,PakY,DeguzmanFR,NandaN,PandeyA,StollaM,BergmeierW,McKenzieSE.PRT-060318,anovelSykinhibitor,preventsheparin-inducedthrombocytopeniaandthrombosisinatransgenicmousemodel.Blood.2011Feb17;117(7):2241-6.doi:10.1182/blood-2010-03-274969.Epub2010Nov18.PubMedPMID:21088136;PubMedCentralPMCID:PMC3568699.

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