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MedKoo Biosciences/Binimetinib (MEK-162)/205531/200mg

Binimetinib,alsoknownasMEK162(ARRY-162),isanoral,highlyselectiveMEKinhibitor.Inpreclinicalstudies,MEK162showedsignificantantitumoractivitiesincelllinesandanimalmodels.MEK162isthefirsttargetedtherapytoshowactivityinpatientswithNRAS-mutatedmelanomaandmightofferanewoptionforacancerwithfeweffectivetreatments.

MedKooCat#:205531
Name:Binimetinib(MEK-162)
CAS#:606143-89-9
ChemicalFormula:C17H15BrF2N4O3
ExactMass:440.02956
MolecularWeight:441.22681
ElementalAnalysis:C,46.28;H,3.43;Br,18.11;F,8.61;N,12.70;O,10.88


Synonym:MEK162;MEK-162;MEK162;ARRY162;ARRY-162;ARRY162;ARRY438162,Binimetinib

IUPAC/ChemicalName:5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.

InChiKey:ACWZRVQXLIRSDF-UHFFFAOYSA-N

InChiCode:InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

SMILESCode:O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:
ViewCoA:currentbatch,Lot#CRB50630

QCData:
ViewQCdata:currentbatch,Lot#CRB50630

SafetyDataSheet(MSDS):
ViewMaterialSafetyDataSheet(MSDS)

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:HamidiH,LuM,ChauK,AndersonL,FejzoM,GintherC,LinnartzR,ZubelA,SlamonDJ,FinnRS.KRASmutationalsubtypeandcopynumberpredictinvitroresponseofhumanpancreaticcancercelllinestoMEKinhibition.BrJCancer.2014Aug28.doi:10.1038/bjc.2014.475.[Epubaheadofprint]PubMedPMID:25167228.

2:RebeccaVW,AliceaGM,ParaisoKH,LawrenceH,GibneyGT,SmalleyKS.VerticalinhibitionoftheMAPKpathwayenhancestherapeuticresponsesinNRAS-mutantmelanoma.PigmentCellMelanomaRes.2014Aug11.doi:10.1111/pcmr.12303.[Epubaheadofprint]PubMedPMID:25130256.

3:Urner-BlochU,UrnerM,StiegerP,GallikerN,WintertonN,ZubelA,Moutouh-deParsevalL,DummerR,GoldingerSM.TransientMEKinhibitor-associatedretinopathyinmetastaticmelanoma.AnnOncol.2014Jul;25(7):1437-41.doi:10.1093/annonc/mdu169.Epub2014May26.PubMedPMID:24864047.

4:Küsters-VandeveldeHV,WillemsenAE,GroenenPJ,KüstersB,LammensM,WesselingP,DjafarihamedaniM,RijntjesJ,DelyeH,WillemsenMA,vanHerpenCM,BlokxWA.ExperimentaltreatmentofNRAS-mutatedneurocutaneousmelanocytosiswithMEK162,aMEK-inhibitor.ActaNeuropatholCommun.2014Apr8;2(1):41.doi:10.1186/2051-5960-2-41.PubMedPMID:24713450;PubMedCentralPMCID:PMC4023633.

5:ThumarJ,ShahbazianD,AzizSA,JilaveanuLB,KlugerHM.MEKtargetinginN-RASmutatedmetastaticmelanoma.MolCancer.2014Mar4;13:45.doi:10.1186/1476-4598-13-45.PubMedPMID:24588908;PubMedCentralPMCID:PMC3945937.

6:GritsmanK,YuzugulluH,VonT,YanH,ClaytonL,FritschC,MairaSM,HollingworthG,ChoiC,KhandanT,PaktinatM,OkabeRO,RobertsTM,ZhaoJJ.HematopoiesisandRAS-drivenmyeloidleukemiadifferentiallyrequirePI3Kisoformp110α.JClinInvest.2014Apr1;124(4):1794-809.doi:10.1172/JCI69927.Epub2014Feb24.PubMedPMID:24569456;PubMedCentralPMCID:PMC3973083.

7:MillerCR,OliverKE,FarleyJH.MEK1/2inhibitorsinthetreatmentofgynecologicmalignancies.GynecolOncol.2014Apr;133(1):128-37.doi:10.1016/j.ygyno.2014.01.008.Epub2014Jan14.Review.PubMedPMID:24434059.

8:ChenX,WuQ,TanL,PorterD,JagerMJ,EmeryC,BastianBC.CombinedPKCandMEKinhibitioninuvealmelanomawithGNAQandGNA11mutations.Oncogene.2013Oct21.doi:10.1038/onc.2013.418.[Epubaheadofprint]PubMedPMID:24141786.

9:DavarD,TarhiniAA,KirkwoodJM.Adjuvantimmunotherapyofmelanomaanddevelopmentofnewapproachesusingtheneoadjuvantapproach.ClinDermatol.2013May-Jun;31(3):237-50.doi:10.1016/j.clindermatol.2012.08.012.Review.Erratumin:ClinDermatol.2013Jul-Aug;31(4):501.PubMedPMID:23608443;PubMedCentralPMCID:PMC3654101.

10:AkinleyeA,FurqanM,MukhiN,RavellaP,LiuD.MEKandtheinhibitors:frombenchtobedside.JHematolOncol.2013Apr12;6:27.doi:10.1186/1756-8722-6-27.Review.PubMedPMID:23587417;PubMedCentralPMCID:PMC3626705.

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