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MedKoo Biosciences/P50515 hydrochloride/406272/2g

P505-15,alsoknownasPRT2607,PRT062607,andBIIB057,isanovel,highlyselective,andorallybioavailablesmallmoleculeSYKinhibitor(SYKIC(50)=1nM)withanti-SYKactivitythatisatleast80-foldgreaterthanitsaffinityforotherkinases.P505-15successfullyinhibitedSYK-mediatedB-cellreceptorsignalinganddecreasedcellviabilityinNHLandCLL.

MedKooCat#:406272
Name:P505-15hydrochloride
CAS#:1370261-97-4(HCl)
ChemicalFormula:C19H24ClN9O
ExactMass:393.20256
MolecularWeight:429.913
ElementalAnalysis:C,53.08;H,5.63;Cl,8.25;N,29.32;O,3.72


RelatedCAS#:1370261-97-4(HCl) 1370261-96-3(freebase)  

Synonym:PRT2607;PRT-2607;PRT2607;PRT062607;PRT-062607;PRT062607;P-505-15;P505-15;P505-15;BIIB057;BIIB-057;BIIB057.

IUPAC/ChemicalName:4-((3-(2H-1,2,3-triazol-2-yl)phenyl)amino)-2-(((1R,2S)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamidehydrochloride

InChiKey:RMNLLPXCNDZJMJ-IDVLALEDSA-N

InChiCode:InChI=1S/C19H23N9O.ClH/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28;/h4-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27);1H/t15-,16+;/m0./s1

SMILESCode:O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)N.[H]Cl


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

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


AdditionalInformation


 


References

1:SpurgeonSE,CoffeyG,FletcherLB,BurkeR,TynerJW,DrukerBJ,BetzA,DeGuzmanF,PakY,BakerD,PandeyA,HollenbachSJ,SinhaU,LoriauxMM.TheselectiveSYKinhibitorP505-15(PRT062607)inhibitsBcellsignalingandfunctioninvitroandinvivoandaugmentstheactivityoffludarabineinchroniclymphocyticleukemia.JPharmacolExpTher.2013Feb;344(2):378-87.doi:10.1124/jpet.112.200832.Epub2012Dec7.PubMedPMID:23220742;PubMedCentralPMCID:PMC3558816.

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

3:CoffeyG,DeGuzmanF,InagakiM,PakY,DelaneySM,IvesD,BetzA,JiaZJ,PandeyA,BakerD,HollenbachSJ,PhillipsDR,SinhaU.Specificinhibitionofspleentyrosinekinasesuppressesleukocyteimmunefunctionandinflammationinanimalmodelsofrheumatoidarthritis.JPharmacolExpTher.2012Feb;340(2):350-9.doi:10.1124/jpet.111.188441.Epub2011Oct31.PubMedPMID:22040680.


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