Cabozantinib-hydrochloride-XL184-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECabozantinibhydrochlorideCat.No.:HY-13016ACASNo.:1817759-42-4Synonyms:XL184hydrochloride;BMS-907351hydrochloride分⼦式:C₂₈H₂₅ClFN₃O₅分⼦量:537.97作⽤靶点:VEGFR;c-Met/HGFR;c-Kit;TAMReceptor;FLT3;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Cabozantinibhydrochloride⼀种⼝服有效的VEGFR2和MET抑制剂，IC50分别为0.035和1.3nM。Cabozantinibhydrochloride对KIT、RET、AXL、TIE2和FLT3有较强的抑制作⽤(IC50=4.6、5.2、7、14.3和11.3nM)。Cabozantinibhydrochloride显⽰出抗⾎管⽣成活性。Cabozantinibhydrochloride可以破坏肿瘤⾎管，促进肿瘤和内⽪细胞凋亡(apoptosis)[1]。IC50&TargetVEGFR2METMETY1248HMETD1246N0.035±0.nM(IC50)1.3±1.2nM(IC50)3.8nM(IC50)11.8nM(IC50)Flt-4Flt-16nM(IC50)12nM(IC50)体外研究CabozantinibhydrochlorideinhibitsphosphorylationofMETandVEGFR2,aswellasKIT,FLT3,andAXLwithIC50valuesof7.8,1.9,5.0,7.5,and42μM,respectively[1].Cabozantinibhydrochloride(4.6nM)inhibitstubuleformationwithnoevidenceofcytotoxicity,withIC50valuesof6.7,5.1,4.1,7.7,and4.7nMinHMVEC,MDA-MB-231,A431,HT1080,andB16F10cells,respectively[1].Cabozantinibhydrochloride(0-370nM,24h)inhibitscellularmigrationandinvasion[1].Cabozantinibhydrochloride(48h)inhibitstumorcellproliferationinavarietyoftumortypes[1].CellProliferationAssayCellLine:SNU-5,Hs746T,SNU-1,SNU-16,MDA-MB-231,U87MG,H441,H69,andPC3cells[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:IncubationTime:48hoursResult:Inhibitedtumorcellproliferation,withIC50of19,9.9,5223,1149,6421,1851,21700,20200,and10800nM,respectively.CellMigrationAssayCellLine:B16F10cells[1]Concentration:0,41,123,and370nMIncubationTime:24hoursResult:PotentlyinhibitedHGF-inducedmigration(IC50=31nM)ofB16F10cells.CellInvasionAssayCellLine:B16F10cells[1]Concentration:0,1.5,14,and123nMIncubationTime:24hoursResult:PotentlyinhibitedHGF-inducedinvasion(IC50=9nM)ofB16F10cells.体内研究Cabozantinibhydrochloride(100mg/kg,Orally,once)inhibitsMETandVEGFR2phosphorylationinmice[1].Cabozantinibhydrochloride(100mg/kg,Orally,once)significantlyincreasestumorhypoxiaandapoptosis[1].Cabozantinibhydrochloride(0-60mg/kg,Orally,oncedailyfor14days)inhibitstumorgrowthinadose-dependentmanner[1].AnimalModel:FemalemicebearingMBA-MB-231tumor(5pergroup)[1]Dosage:0,100mg/kgAdministration:Orally,onceResult:InhibitedMETandVEGFR2phosphorylation.AnimalModel:MicebearingMBA-MB-231tumor[1]Dosage:1,3,10,30,60mg/kgAdministration:Orally,oncedailyfor14days2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Inhibitedtumorgrowthinadose-dependentmanner.户使⽤本产品发表的科研⽂献•CancerDiscov.2021Jan;11(1):126-141.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•Biomaterials.16September2022.•JPharmAnal.2021Jun19.•CancerLett.2019Apr10;447:105-114.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YakesFM,etal.Cabozantinib(XL184),anovelMETandVEGFR2inhibitor,simultaneouslysuppressesmetastasis,angiogenesis,andtumorgrowth.MolCancerTher,2011,10(12),2298-2308.[2].YouWK,etal.VEGFandc-Metblockadeamplifyangiogenesisinhibitioninpancreaticisletcancer.CancerRes,2011,71(14),4758-4768.McePdfHeightCaution:Producthasno