Tivozanib-hydrate-AV-951-hydrate-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemETivozanibhydrateCat.No.:HY-112467CASNo.:682745-40-0Synonyms:AV-951hydrate;KRN951hydrate分子式:C₂₂H₂₁ClN₄O₆分子量:472.88作用靶点:VEGFR作用通路:ProteinTyrosineKinase/RTK储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Tivozanibhydrate(AV-951hydrate;KRN951hydrate)是Tivozanib(HY-10977)的水合物形式。Tivozanibhydrate是口服有效的血管内皮生长因子受体(VEGFR)-1,23抑制剂，IC50为30，6.5和15nM。Tivozanibhydrate具有抗肿瘤活性[1]。IC50&TargetVEGFR2VEGFR3VEGFR16.5nM(IC50)15nM(IC50)30nM(IC50)体外研究TivozanibhydrateinhibitsthephosphorylationofVEGFR-1,VEGFR-2,andVEGFR-3,withIC50sof0.16-0.24nM[1].Tivozanibhydrate(0-100nM,24h)inhibitsVEGF-inducedproliferationofHUVECswithIC50of0.67nM,andmigrationofHUVECsindose-dependentmanner[1].Tivozanibhydrate(0-300nM,1h)selectivelyinhibitstheVEGF-stimulatedphosphorylationofMAPKsinendothelialcellsligand-dependently,withIC50sof0.13and0.18nMforERK1andERK2,respectively[1].CellProliferationAssay[1]CellLine:HUVECsConcentration:0-100nMIncubationTime:24hResult:Inhibitedproliferation.1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECellMigrationAssay[1]CellLine:HUVECsConcentration:0-100nMIncubationTime:22hResult:Inhibitedmigration.WesternBlotAnalysis[1]CellLine:HUVECsConcentration:0-300nMIncubationTime:1hResult:InhibitedVEGR-dependentphosphorylationofERK1andERK2.体内研究Tivozanibhydrate(0.04-1mg/kg,pofor14days)exhibitsantitumorefficacyagainstbreast,colon,hepatic,lung,ovarian,pancreatic,andprostatecancerinmodel[1].Tivozanibhydrate(0.2-1mg/kg,pofor21days)reversiblysuppressesvascularpermeabilityandangiogenesisinCalu-6tumorbearingratsmodel[1].Tivozanibhydrate(5mg/kg,po,singledose)revealsaAUCinfof44.5μg·h/mL,Cmaxof2823ng/mLinathymicmicemodel[1].AnimalModel:Calu-6tumorbearingathymicmicemodel[1]Dosage:0.04-1mg/kg/dayAdministration:p.o.,for14-21daysResult:Inhibitedtumorgrowth,angiogenesisandvascularpermeability.客户使用本产品发表的科研文献SciTranslMed.2018Jul18;10(450).pii:eaaq1093.CancerCellInt.2021Jun5;21(1):291.Pharmaceuticals.2023,16(2),295.TechnicalUniversityofMunich.24.01.2018.Patent.US20170349880A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemENakamuraK,etal.,KRN951,ahighlypotentinhibitorofvascularendothelialgrowthfactorreceptortyrosinekinases,hasantitumoractivitiesandaffectsfunctionalvascularproperties.CancerRes.2006Sep15;66(18):9134-42.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic