BI-853520-IN-10018-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBI-853520Cat.No.:HY-122844CASNo.:1227948-82-4Synonyms:IN-10018分?式:C??H??F?N?O?分?量:588.55作?靶點(diǎn):FAK作?通路:ProteinTyrosineKinase/RTK儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性BI853520(IN-10018)?種具有?服活性的粘附斑激酶(FAK)強(qiáng)效抑制劑(重組FAKIC50=1nM)，BI853520表現(xiàn)出對(duì)癌細(xì)胞的抗增殖活性。體外研究BI853520(0-3μM;2h)inhibitscancercellsgrowth[2].BI853520(0-30μM;4-6d)repressestumorcellproliferationandinvasiononlyin3Dculture[1].BI853520(0-10μM;24h)repressesY397-FAKautophosphorylation[1].BI853520(0.1μM;96h)showsafastandpotentinhibitionofFAKinthishighlymetastaticmurinebreastcancercellline[1].CellViabilityAssay[2]CellLine:PC-3cellsConcentration:0-3μMIncubationTime:2hoursResult:Resultedinaconcentration-dependentreductionofthesignalwithamedianEC50valueof1?nM.CellProliferationAssay[1]CellLine:4T1,Py2T,andPy2T-LTcells1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:0-30μMIncubationTime:4-6daysResult:Indicatedthatthespecificinhibitionofcellproliferationandinvasionatlowdosesisfunctionalonlyinthree-dimensionalcellcultureconditions,whereascellsculturedonplasticonlyrespondtoBI853520atveryhigh,toxicdoses.WesternBlotAnalysis[1]CellLine:4T1,Py2T,andPy2T-LTcellsConcentration:0-10μMIncubationTime:24hoursResult:ReducedY397-FAKautophosphorylationinallcelltypes.WesternBlotAnalysis[1]CellLine:4T1,Py2T,andPy2T-LTcellsConcentration:0.1μMIncubationTime:96hoursResult:DecreasedY397-FAKautophosphorylationfollowing0.1?μMBI853520treatmentoccurredwithin10?minandwassubstantiallyreducedatleastforthefollowing48?h.體內(nèi)研究BI853520(oralgavage;50mg/kg;oncedaily;0-8weeks)treatmentsignificantlysuppressesprimarytumorgrowthofallthreecelllinesinvivo[1].AnimalModel:FVB/N,Balb/c,orimmunodeficientnude(nu/nu)micetransplantedwithPy2T,4T1,orMTflECadcells,respectively[1]Dosage:50mg/kgAdministration:Oralgavage;50mg/kg;oncedaily;0-8weeksResult:Decreasedtumorvolumesignificantlyovertime.REFERENCES[1].StefanieTiede,etal.TheFAKinhibitorBI853520exertsanti-tumoreffectsinbreastcancer.Oncogenesis.2018Sep20;7(9):73.[2].UlrichAHirt,etal.EfficacyofthehighlyselectivefocaladhesionkinaseinhibitorBI853520inadenocarcinomaxenograftmodelsislinkedtoamesenchymaltumorphenotype.Oncogenesis.2018Feb23;7(2):21.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica