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MedKoo Biosciences/G-573/406200/5g

G-573isanallostericinhibitorofMEKthatisbothpotentandselective.TheIC(50)valueforpERKinhibitioninHCT116tumoursbyG-573wasestimatedtobe0.406 µM.TheIC(50)valuesfortumourgrowthinhibitioninHCT116andH2122wereestimatedtobe3.43and2.56 µM,respectively.ED(50)estimatesinHCT116andH2122mousexenograftmodelswereestimatedtobe~4.6and1.9 mg/kg/day,respectively.

MedKooCat#:406200
Name:G-573
CAS#:22868-35-5
ChemicalFormula:C13H9ClN2
ExactMass:228.04543
MolecularWeight:228.68
ElementalAnalysis:C,68.28;H,3.97;Cl,15.50;N,12.25


Synonym:G573;G-573;G573.

IUPAC/ChemicalName:2-(3-chlorophenyl)-1H-benzo[d]imidazole

InChiKey:BGYHTIIVIGGCIF-UHFFFAOYSA-N

InChiCode:InChI=1S/C13H9ClN2/c14-10-5-3-4-9(8-10)13-15-11-6-1-2-7-12(11)16-13/h1-8H,(H,15,16)

SMILESCode:ClC1=CC(C2=NC3=CC=CC=C3N2)=CC=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:HatzivassiliouG,HalingJR,ChenH,SongK,PriceS,HealdR,HewittJF,Zak M,PeckA,OrrC,MerchantM,HoeflichKP,ChanJ,LuohSM,AndersonDJ,LudlamMJ,WiesmannC,UltschM,FriedmanLS,MalekS,BelvinM.MechanismofMEKinhibitiondeterminesefficacyinmutantKRAS-versusBRAF-drivencancers.Nature.2013Sep12;501(7466):232-6.doi:10.1038/nature12441.Epub2013Aug11. Erratumin:Nature.2013Oct10;502(7470):258.PubMedPMID:23934108.

2:ChooEF,BelvinM,ChanJ,HoeflichK,OrrC,RobargeK,YangX,ZakM,Boggs J.Preclinicaldispositionandpharmacokinetics-pharmacodynamicmodelingofbioMarkerresponseandtumourgrowthinhibitioninxenograftmousemodelsofG-573,aMEKinhibitor.Xenobiotica.2010Nov;40(11):751-62.doi:10.3109/00498254.2010.514365.PubMedPMID:20836753.

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