MK-8745isanovelAurora-Aspecificinhibitor.MK8745inducedapoptoticcelldeathinap53-dependentmannerwhentestedinvitroincelllinesofmultiplelineages.Exposureofp53wild-typecellstoMK8745resultedintheinductionofp53phosphorylation(ser15)andanincreaseinp53proteinexpression.p53-dependentapoptosisbyMK8745wasfurtherconfirmedinHCT116p53(-/-)cellstransfectedwithwild-typep53.(source:CellCycle.2012Feb15;11(4):807-17.)

MedKooCat#:406251
Name:MK-8745
CAS#:885325-71-3
ChemicalFormula:C20H19ClFN5OS
ExactMass:431.09829
MolecularWeight:431.91416
ElementalAnalysis:C,55.62;H,4.43;Cl,8.21;F,4.40;N,16.21;O,3.70;S,7.42


Synonym:MK-8745;MK8745;MK8745.

IUPAC/ChemicalName:(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone.

InChiKey:YCRFPWKUUNKNDN-UHFFFAOYSA-N

InChiCode:InChI=1S/C20H19ClFN5OS/c21-16-5-2-4-15(18(16)22)19(28)27-10-8-26(9-11-27)13-14-3-1-6-17(24-14)25-20-23-7-12-29-20/h1-7,12H,8-11,13H2,(H,23,24,25)

SMILESCode:O=C(C1=CC=CC(Cl)=C1F)N2CCN(CC3=NC(NC4=NC=CS4)=CC=C3)CC2


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:ShionomeY,YanL,LiuS,SaekiT,OuchiT.Integrityofp53associatedpathwaysdeterminesinductionofapoptosisoftumorcellsresistanttoAurora-Akinaseinhibitors.PLoSOne.2013;8(1):e55457.doi:10.1371/journal.pone.0055457.Epub2013Jan31.PubMedPMID:23383195;PubMedCentralPMCID:PMC3561291.

2:NairJS,HoAL,SchwartzGK.TheinductionofpolyploidyorapoptosisbytheAuroraAkinaseinhibitorMK8745isp53-dependent.CellCycle.2012Feb15;11(4):807-17.doi:10.4161/cc.11.4.19323.Epub2012Feb15.PubMedPMID:22293494;PubMedCentralPMCID:PMC3318110.

3:ChowdhuryA,ChowdhuryS,TsaiMY.AnovelAurorakinaseAinhibitorMK-8745predictsTPX2asatherapeuticbioMarkerinnon-Hodgkinlymphomacelllines.LeukLymphoma.2012Mar;53(3):462-71.doi:10.3109/10428194.2011.619018.Epub2011Oct24.PubMedPMID:21879811.