GW6604isapotentandselectiveALK-5inhibitorwithpotentanticanceractivity.GW6604isalsoaTGF-betasignalingpathwayinhibitor.Invitro,GW6604inhibitedautophosphorylationofALK5withanIC(50)of140nMandinacellularassayinhibitedTGF-beta-inducedtranscriptionofPAI-1(IC(50):500nM).Invivo,GW6604(40mgkg(-1)p.o.)increasedliverregenerationinTGF-beta-overexpressingmice,whichhadundergonepartialhepatectomy.Inanacutemodelofliverdisease,GW6604reducedby80%theexpressionofcollagenIA1.InhibitionofALK5couldbeanattractivenewapproachtotreatmentofliverfibroticdiseasesbybothpreventingmatrixdepositionandpromotinghepatocyteregeneration.(BrJPharmacol.2005May;145(2):166-77.).

MedKooCat#:406614
Name:GW6604
CAS#:452342-37-9
ChemicalFormula:C19H14N4
ExactMass:298.12185
MolecularWeight:298.34126
ElementalAnalysis:C,76.49;H,4.73;N,18.78


Synonym:GW6604;GW-6604;GW6604.

IUPAC/ChemicalName:2-phenyl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine

InChiKey:BDCBRQYHYNUWAM-UHFFFAOYSA-N

InChiCode:InChI=1S/C19H14N4/c1-2-6-14(7-3-1)18-12-15(9-11-21-18)16-13-22-23-19(16)17-8-4-5-10-20-17/h1-13H,(H,22,23)

SMILESCode:C1(C2=CC=CC=C2)=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C1


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:CiayADIR,KelsoGF,PotdarMK,HarrisSJ,WaltonKL,HarrisonCA,HearnMT.IdentificationofproteinbindingpartnersofALK-5kinaseinhibitors.BioorgMedChem.2013Nov1;21(21):6496-500.doi:10.1016/j.bmc.2013.08.038.Epub2013Aug29.PubMedPMID:24055074.

2:deGouvilleAC,HuetS.InhibitionofALK5asanewapproachtotreatliverfibroticdiseases.DrugNewsPerspect.2006Mar;19(2):85-90.Review.PubMedPMID:16628263.

3:deGouvilleAC,BoullayV,KrysaG,PilotJ,BrusqJM,LoriolleF,GauthierJM,PapworthSA,LarozeA,GellibertF,HuetS.InhibitionofTGF-betasignalingbyanALK5inhibitorprotectsratsfromdimethylnitrosamine-inducedliverfibrosis.BrJPharmacol.2005May;145(2):166-77.PubMedPMID:15723089;PubMedCentralPMCID:PMC1576127.