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主营:抗癌化学试剂和激酶抑制剂
℡ 4000-520-616
℡ 4000-520-616
MedKoo Biosciences/Golvatinib/201072/10g
产品编号:201072-10g
市  场 价:¥119000.00
场      地:美国(厂家直采)
产品分类: 生化试剂>其他>其他试剂>
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电话号码:4000-520-616
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美  元  价:$5950.00
品      牌: MedKoo
公      司:MedKoo Biosciences, Inc
公司分类:
MedKoo Biosciences/Golvatinib/201072/10g
商品介绍
Golvatinib,alsoknownasE7050,isanorallybioavailabledualkinaseinhibitorofc-Met(hepatocytegrowthfactorreceptor)andVEGFR-2(vascularendothelialgrowthfactorreceptor-2)tyrosinekinaseswithpotentialantineoplasticactivity.c-Met/VEGFRkinaseinhibitorE7050bindstoandinhibitstheactivitiesofbothc-MetandVEGFR-2,whichmayinhibittumorcellgrowthandsurvivaloftumorcellsthatoverexpressthesereceptortyrosinekinases.c-MetandVEGFR-2areupregulatedinavarietyofvarioustumorcelltypesandplayimportantrolesintumorcellgrowth,migrationandangiogenesis.

MedKooCat#:201072
Name:Golvatinib
CAS#:928037-13-2
ChemicalFormula:C33H37F2N7O4
ExactMass:633.28751
MolecularWeight:633.69
ElementalAnalysis:C,62.55;H,5.89;F,6.00;N,15.47;O,10.10


Synonym: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-dicarboxamide

InChiKey:BWEYRDZIIMFBJR-UHFFFAOYSA-N

InChiCode: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=C6


TechnicalData

Appearance:
whitesolidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:
ViewcurrentbatchofCoA

QCData:
ViewNMR,ViewHPLC,ViewMS

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

E7050isthefirstkinaseinhibitorwithdualactionagainstbothc-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:
)


References

1: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.

品牌介绍
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中    文美帝药库医药科技公司创立于2008年总部位于美国东海岸
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