MedKoo Biosciences/Brigatinibanalog/205765/5g

Brigatinib-analogisanorallyactive,potentandselectiveanaplasticlymphomakinase(ALK)andtheepidermalgrowthfactorreceptor(EGFR)inhibitor.Brigatinib-analogisstructurallyrelatedtoBrigatinib(AP-26113).Brigatinib-analogbindstoandinhibitsALKkinaseandALKfusionproteinsaswellasEGFRandmutantforms.ThisleadstotheinhibitionofALKkinaseandEGFRkinase,disruptstheirsignalingpathwaysandeventuallyinhibitstumorcellgrowthinsusceptibletumorcells.

MedKooCat#:205765
Name:Brigatinib-analog
CAS#:1197958-12-5(Brigatinibanalog)
ChemicalFormula:C26H34ClN6O2P
ExactMass:528.21694
MolecularWeight:529.01
ElementalAnalysis:C,59.03;H,6.48;Cl,6.70;N,15.89;O,6.05;P,5.85

RelatedCAS#:1197958-12-5(Brigatinibanalog) 1197953-54-0(Brigatinib)

Synonym:AP26113-analog;AP-26113-analog;AP26113-analog,Brigatinib-analog

IUPAC/ChemicalName:(2-((5-chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphineoxide

InChiKey:OVDSPTSBIQCAIN-UHFFFAOYSA-N

InChiCode:InChI=1S/C26H34ClN6O2P/c1-32(2)18-12-14-33(15-13-18)19-10-11-21(23(16-19)35-3)30-26-28-17-20(27)25(31-26)29-22-8-6-7-9-24(22)36(4,5)34/h6-11,16-18H,12-15H2,1-5H3,(H2,28,29,30,31)

SMILESCode:CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCC(N(C)C)CC4)C=C3OC)=NC=C2Cl)=O

TechnicalData

Appearance:

whitesolidpowder

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

Brigatinib-Analogwasintroducedtotheresearchcommunityduetowronginformationpublishedinthefollowingwell-knownresources.thewronginformationhadbeenmisleadmanyreagentvendorsincludedMedKoo.

ThefollowingresourceshavepublishedawrongstructureforBrigatinib(AP-26113)

1.Somepapers
SuchasOncoTargetsTher.2014Mar5;7:375-85.,http://www.ncbi.nlm.nih.gov/pubmed/24623980)

2.wikipedia(https://en.wikipedia.org/wiki/Brigatinib,lastvisitedon12/9/2015).

3.Sci-FinderScholarDatabase:BeforeDecember2015,Sci-FinderScholarDatabasealsowronglylistedCAS#1197958-12-5asBrigatinib(AP26113).NowSci-FinderScholarDatabasehascorrected.

4.Pubchem:https://pubchem.ncbi.nlm.nih.gov/compound/ap26113

References

1:RossiA,MaioneP,SaccoPC,SgambatoA,CasaluceF,FerraraML,PalazzoloG,CiardielloF,GridelliC.ALKinhibitorsandadvancednon-smallcelllungcancer(review).IntJOncol.2014Aug;45(2):499-508.doi:10.3892/ijo.2014.2475.Epub2014May29.PubMedPMID:24889366.

2:IwamaE,OkamotoI,HaradaT,TakayamaK,NakanishiY.Developmentofanaplasticlymphomakinase(ALK)inhibitorsandmoleculardiagnosisinALKrearrangement-positivelungcancer.OncoTargetsTher.2014Mar5;7:375-85.doi:10.2147/OTT.S38868.eCollection2014.Review.PubMedPMID:24623980;PubMedCentralPMCID:PMC3949762.

3:PerezCA,VelezM,RaezLE,SantosES.Overcomingtheresistancetocrizotinibinpatientswithnon-smallcelllungcancerharboringEML4/ALKtranslocation.LungCancer.2014May;84(2):110-5.doi:10.1016/j.lungcan.2014.02.001.Epub2014Feb8.PubMedPMID:24598368.

4:SolomonB,WilnerKD,ShawAT.Currentstatusoftargetedtherapyforanaplasticlymphomakinase-rearrangednon-smallcelllungcancer.ClinPharmacolTher.2014Jan;95(1):15-23.doi:10.1038/clpt.2013.200.Epub2013Oct3.Review.PubMedPMID:24091716.

5:YuHA,RielyGJ.Second-generationepidermalgrowthfactorreceptortyrosinekinaseinhibitorsinlungcancers.JNatlComprCancNetw.2013Feb1;11(2):161-9.PubMedPMID:23411383;PubMedCentralPMCID:PMC3673302.

6:CecconM,MologniL,BissonW,ScapozzaL,Gambacorti-PasseriniC.Crizotinib-resistantNPM-ALKmutantsconferdifferentialsensitivitytounrelatedAlkinhibitors.MolCancerRes.2013Feb;11(2):122-32.doi:10.1158/1541-7786.MCR-12-0569.Epub2012Dec13.PubMedPMID:23239810.

7:KatayamaR,KhanTM,BenesC,LifshitsE,EbiH,RiveraVM,ShakespeareWC,IafrateAJ,EngelmanJA,ShawAT.Therapeuticstrategiestoovercomecrizotinibresistanceinnon-smallcelllungcancersharboringthefusiononcogeneEML4-ALK.ProcNatlAcadSciUSA.2011May3;108(18):7535-40.doi:10.1073/pnas.1019559108.Epub2011Apr18.PubMedPMID:21502504;PubMedCentralPMCID:PMC3088626.

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MedKoo Biosciences/Brigatinibanalog/205765/5g

TechnicalData

AdditionalInformation

References