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MedKoo Biosciences/Golvatinib/201072/200mg

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Golvatinib,alsoknownasE7050,isanorallybioavailabledualkinaseinhibitorofc-Met(hepatocytegrowthfactorreceptor)andVEGFR-2(vascularendothelialgrowthfactorreceptor-2)tyrosinekinaseswithpotentialantineoplasticactivity.c-Met/VEGFRkinaseinhibitorE7050bindstoandinhibitstheactivitiesofbothc-MetandVEGFR-2,whichmayinhibittumorcellgrowthandsurvivaloftumorcellsthatoverexpressthesereceptortyrosinekinases.c-MetandVEGFR-2areupregulatedinavarietyofvarioustumorcelltypesandplayimportantrolesintumorcellgrowth,migrationandangiogenesis.MedKooCat#:201072Name:GolvatinibCAS#:928037-13-2ChemicalFormula:C33H37F2N7O4ExactMass:633.28751MolecularWeight:633.69ElementalAnalysis:C,62.55;H,5.89;F,6.00;N,15.47;O,10.10Synonym:E7050;E-7050;E7050;Golvatinib.IUPAC/ChemicalName:N-(2-fluoro-4-((2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamideInChiKey:BWEYRDZIIMFBJR-UHFFFAOYSA-NInChiCode:InChI=1S/C33H37F2N7O4/c1-39-16-18-40(19-17-39)23-9-14-41(15-10-23)32(45)38-29-21-26(8-13-37-29)46-25-6-7-28(27(35)20-25)42(24-4-2-22(34)3-5-24)31(44)33(11-12-33)30(36)43/h2-8,13,20-21,23H,9-12,14-19H2,1H3,(H2,36,43)(H,37,38,45)SMILESCode:O=C(C1(C(N)=O)CC1)N(C2=CC=C(OC3=CC(NC(N4CCC(N5CCN(C)CC5)CC4)=O)=NC=C3)C=C2F)C6=CC=C(F)C=C6TechnicalDataAppearance:whitesolidpowderPurity:>98%(orrefertotheCertificateofAnalysis)CertificateofAnalysis:ViewcurrentbatchofCoAQCData:ViewNMR,ViewHPLC,ViewMSSafetyDataSheet(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:293490AdditionalInformationE7050isthefirstkinaseinhibitorwithdualactionagainstbothc-MetandVEGFR-2.ThedualinhibitoryactivityofE7050againsttumorgrowthandangiogenesisresultsindrastictumorregressionanddisappearanceandalsoprolongationofLifespanwithoutadverseeffects. E7050iscurrentlyunderevaluationinaphaseIclinicaltrial. (CancerSci.2010Jan;101(1):210-5.Epub2009Sep2.).E7050isthefirstkinaseinhibitorwithdualactionagainstbothc-MetandVEGFR-2.ThedualinhibitoryactivityofE7050againsttumorgrowthandangiogenesisresultsindrastictumorregressionanddisappearanceandalsoprolongationoflifespanwithoutadverseeffects. E7050iscurrentlyunderevaluationinaphaseIclinicaltrial. (). E7050circumventedresistancetoallofthereversIBLe,irreversible,andmutant-selectiveEGFR-TKIsinducedbyexogenousand/orendogenousHGFinEGFRmutantlungcancercelllines,byblockingtheMet/Gab1/PI3K/Aktpathwayinvitro.E7050alsopreventedtheemergenceofgefitinib-resistantHCC827cellsinducedbycontinuousexposuretoHGF.Intheinvivomodel,E7050plusgefitinibresultedinmarkedregressionoftumorgrowthassociatedwithinhibitionofAktphosphorylationincancercells.CONCLUSIONS:AnewMetkinaseinhibitor,E7050,reversesthethreeHGF-inducedmechanismsofgefitinibresistance,suggestingthatE7050mayovercomeHGF-inducedresistancetogefitinibandnext-generationEGFR-TKIs.(source:ClinCancerRes.2012Mar15;18(6):1663-71.Epub2012Feb8.)E7050circumventedresistancetoallofthereversible,irreversible,andmutant-selectiveEGFR-TKIsinducedbyexogenousand/orendogenousHGFinEGFRmutantlungcancercelllines,byblockingtheMet/Gab1/PI3K/Aktpathwayinvitro.E7050alsopreventedtheemergenceofgefitinib-resistantHCC827cellsinducedbycontinuousexposuretoHGF.Intheinvivomodel,E7050plusgefitinibresultedinmarkedregressionoftumorgrowthassociatedwithinhibitionofAktphosphorylationincancercells.CONCLUSIONS:AnewMetkinaseinhibitor,E7050,reversesthethreeHGF-inducedmechanismsofgefitinibresistance,suggestingthatE7050mayovercomeHGF-inducedresistancetogefitinibandnext-generationEGFR-TKIs.(source:)References1:NakagawaT,TakeuchiS,YamadaT,NanjoS,IshikawaD,SanoT,KitaK,NakamuraT,MatsumotoK,SudaK,MitsudomiT,SekidoY,UenakaT,YanoS.CombinedTherapywithMutant-SelectiveEGFRInhibitorandMetKinaseInhibitorforOvercomingErlotinibResistanceinEGFR-MutantLungCancer.MolCancerTher.2012Oct;11(10):2149-57.doi:10.1158/1535-7163.MCT-12-0195.Epub2012Jul25.PubMedPMID:22844075.2:TakeuchiS,WangW,LiQ,YamadaT,KitaK,DonevIS,NakamuraT,MatsumotoK,ShimizuE,NishiokaY,SoneS,NakagawaT,UenakaT,YanoS.DualinhibitionofMetkinaseandangiogenesistoovercomeHGF-inducedEGFR-TKIresistanceinEGFRmutantlungcancer.AmJPathol.2012Sep;181(3):1034-43.doi:10.1016/j.ajpath.2012.05.023.Epub2012Jul9.PubMedPMID:22789825.3:WangW,LiQ,TakeuchiS,YamadaT,KoizumiH,NakamuraT,MatsumotoK,MukaidaN,NishiokaY,SoneS,NakagawaT,UenakaT,YanoS.MetkinaseinhibitorE7050reversesthreedifferentmechanismsofhepatocytegrowthfactor-inducedtyrosinekinaseinhibitorresistanceinEGFRmutantlungcancer.ClinCancerRes.2012Mar15;18(6):1663-71.Epub2012Feb8.PubMedPMID:22317763.4:GreenDR.'Tit-for-tat'incellBIOLOGy.NatRevMolCellBiol.2011Feb;12(2):73.PubMedPMID:21252991.5:NakagawaT,TohyamaO,YamaguchiA,MatsushimaT,TakahashiK,FunasakaS,ShirotoriS,AsadaM,ObaishiH.E7050:adualc-MetandVEGFR-2tyrosinekinaseinhibitorpromotestumorregressionandprolongssurvivalinmousexenograftmodels.CancerSci.2010Jan;101(1):210-5.Epub2009Sep2.PubMedPMID:19832844.

MedKoo 美帝药库公司以药物化学合成技术为核心，密切结合全球抗癌新药研发领域中的新技术、新理论、新趋势和新的发展方向，不断推出抗癌化合物新品种。。

美帝药库MedKoo将在中国建立药物化学合成生产基地和多个现代化药物化合物存储仓库。

美帝药库的药物化合物来源于以下几个渠道：自主合成、委托化学合成、合作伙伴、和从国内外市场上选购。

MedKoo美帝药库的抗癌分子库

MedKoo的目标是打造全球规模最大、品种最多、类别最全和质量最好的小分子抗癌化合物库。MedKoo的抗癌药库将由下列5个分子库组成：

（1）上市抗癌药库：该库将含有大约100个全球已批准上市的小分子抗癌化合物；

（2）抗癌候选药物库：该分子库含有大约400个世界各国正在临床研究中抗癌小分子候选药物；

（3）同系抗癌分子库：该分子库将含有多个化学结构类似或抗癌机制类似的分子包；

（4）抗癌分子预制模块库：该库主要含有用于组建抗癌目标分子的分子模块包；

（5）同位素标记抗癌分子库。