Olmutinib,alsoknownasHM61713andBI-1482694,isapotentsmallmoleculeinhibitorofBruton"styrosinekinase(BTK).BTKisamemberoftheTecfamilyofnon-receptorproteintyrosinekinases.BTKismostlyexpressedinhematopoieticcellssuchasBcells,mastcellsandmacrophages.BTKplayskeyrolesinmultiplecellsignalingpathwaysincludingB-CellReceptor(BCR)andFcreceptor(FcR)signalingcascadesandisanessentialmediatornotonlyinB-celldependentbutalsoinmyeloidcelldependentinflammatoryarthritis.HM71224hasbeenselectedasanoveltherapeuticagentforthetreatmentofautoimmunediseasessuchasRA.MedKooCat#:206083Name:OlmutinibfreebaseCAS#:1353550-13-6(freebase)ChemicalFormula:C26H26N6O2SExactMass:486.18379MolecularWeight:486.59ElementalAnalysis:C,64.18;H,5.39;N,17.27;O,6.58;S,6.59Synonym:HM61713;HM61713;HM-61713;BI1482694;BI-1482694;BI1482694;Olmutinib.IUPAC/ChemicalName:N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamideInChiKey:FDMQDKQUTRLUBU-UHFFFAOYSA-NInChiCode:InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h4-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)SMILESCode:C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=OTechnicalDataAppearance:LightyellowsolidpowderPurity:>98%(orrefertotheCertificateofAnalysis)CertificateofAnalysis:ViewCoA:currentbatch,Lot#CBT60315QCData:ViewQCdata:currentbatch,Lot#CBT60315SafetyDataSheet(MSDS):ViewMaterialSafetyDataSheet(MSDS)ShippingCondition:Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.StorageCondition:Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).Solubility:SolubleinDMSO,notinwaterShelfLife:>2yearsifstoredproperlyDrugFormulation:ThisdrugmaybeformulatedinDMSOStockSolutionStorage:0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).HarmonizedSystemCode:293490AdditionalInformationRelatedCAS#1353550-13-6(freebase);1842366-97-5(HCl).1802181-20-9(deletedCAS#)Note:Olmutinibwaspreviouslymistakelycitedas"HM71224".Asof9/12/2016,therearemanyvendorstillcit   References1:ParkK,HanJY,KimDW,BazhenovaLA,OuSH,PangYK,HinHS,JuanO,SonJ,JänneP.190TiP:ELUXA1:PhaseIIstudyofBI1482694(HM61713)inpatients(pts)withT790M-positivenon-smallcelllungcancer(NSCLC)aftertreatmentwithanepidermalgrowthfactorreceptortyrosinekinaseinhibitor(EGFRTKI).JThoracOncol.2016Apr;11(4Suppl):S139.doi:10.1016/S1556-0864(16)30299-4.Epub2016Apr15.PubMedPMID:27198328.2:ParkK,LeeJS,HanJY,LeeKH,KimJH,ChoEK,ChoJY,MinYJ,KimJS,KimDW.1300:EfficacyandsafetyofBI1482694(HM61713),anEGFRmutant-specificinhibitor,inT790M-positiveNSCLCattherecommendedphaseIIdose.JThoracOncol.2016Apr;11(4Suppl):S113.doi:10.1016/S1556-0864(16)30243-X.Epub2016Apr15.PubMedPMID:27198272.3:WangS,CangS,LiuD.Third-generationinhibitorstargetingEGFRT790Mmutationinadvancednon-smallcelllungcancer.JHematolOncol.2016Apr12;9:34.doi:10.1186/s13045-016-0268-z.Review.PubMedPMID:27071706;PubMedCentralPMCID:PMC4830020.4:TanCS,ChoBC,SooRA.Next-generationepidermalgrowthfactorreceptortyrosinekinaseinhibitorsinepidermalgrowthfactorreceptor-mutantnon-smallcelllungcancer.LungCancer.2016Mar;93:59-68.doi:10.1016/j.lungcan.2016.01.003.Epub2016Jan8.Review.PubMedPMID:26898616.5:SongHN,JungKS,YooKH,ChoJ,LeeJY,LimSH,KimHS,SunJM,LeeSH,AhnJS,ParkK,ChoiYL,ParkW,AhnMJ.AcquiredC797SMutationuponTreatmentwithaT790M-SpecificThird-GenerationEGFRInhibitor(HM61713)inNon-SmallCellLungCancer.JThoracOncol.2016Apr;11(4):e45-7.doi:10.1016/j.jtho.2015.12.093.Epub2015Dec31.PubMedPMID:26749488.6:PirkerR.Third-generationepidermalgrowthfactorreceptortyrosinekinaseinhibitorsinadvancednonsmallcelllungcancer.CurrOpinOncol.2016Mar;28(2):115-21.doi:10.1097/CCO.0000000000000260.PubMedPMID:26720671.7:OuSH,SooRA.Dacomitinibinlungcancer:a"lostgeneration"EGFRtyrosine-kinaseinhibitorfromabygoneera?DrugDesDevelTher.2015Oct15;9:5641-53.doi:10.2147/DDDT.S52787.eCollection2015.Review.PubMedPMID:26508839;PubMedCentralPMCID:PMC4610796.8:TartaroneA,LeroseR.Clinicalapproachestotreatpatientswithnon-smallcelllungcancerandepidermalgrowthfactorreceptortyrosinekinaseinhibitoracquiredresistance.TherAdvRespirDis.2015Oct;9(5):242-50.doi:10.1177/1753465815587820.Epub2015May27.Review.PubMedPMID:26016841.9:WangH,GuoR,ZhangL.[TKIResistanceforT790MMutation].ZhongguoFeiAiZaZhi.2015Apr;18(4):245-50.doi:10.3779/j.issn.1009-3419.2015.04.10.Review.Chinese.PubMedPMID:25936890.10:LiaoBC,LinCC,YangJC.Secondandthird-generationepidermalgrowthfactorreceptortyrosinekinaseinhibitorsinadvancednonsmallcelllungcancer.CurrOpinOncol.2015Mar;27(2):94-101.doi:10.1097/CCO.0000000000000164.Review.PubMedPMID:25611025.11:StinchcombeTE.Recentadvancesinthetreatmentofnon-smallcellandsmallcelllungcancer.F1000PrimeRep.2014Dec1;6:117.doi:10.12703/P6-117.eCollection2014.Review.PubMedPMID:25580271;PubMedCentralPMCID:PMC4251418.12:SteuerCE,KhuriFR,RamalingamSS.Thenextgenerationofepidermalgrowthfactorreceptortyrosinekinaseinhibitorsinthetreatmentoflungcancer.Canc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