Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVEGFR-2-IN-58Cat.No.:HY-170366分?式:C??H??ClN?O分?量:397.86作?靶點:VEGFR;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性VEGFR-2-IN-58(Compound7b)抑制VEGFR-2(HY-P72429)，IC50為42.5nM。VEGFR-2-IN-58對癌細胞具有選擇性細胞毒性。VEGFR-2-IN-58在癌細胞中顯?G2/M期細胞周期阻滯。VEGFR-2-IN-58誘導(dǎo)細胞凋亡(Apoptosis)，增加BAX表達，降低Bcl2表達。VEGFR-2-IN-58抑制癌細胞傷?閉合。IC50&TargetVEGFR242.5nM(IC50)體外研究VEGFR-2-IN-58inhibitsHepG2,MCF-7,A549,HT-29,PC3andWI-38cellsproliferationwithIC50sof7.28,6.72,6.66,8.51,14.5,30μM,respectively[1].VEGFR-2-IN-58(8.51μM,24h)showscellulargrowtharrestattheG2/MphaseandinducesapoptosisintheHT-29cellline[1].VEGFR-2-IN-58(0.85,4.26μM,48h)exertsanoticeableinhibitioninwoundclosureinHT-29cells[1].WesternBlotAnalysis[1]CellLine:HT-29cellsConcentration:0.85,4.26,8.51μMIncubationTime:24hResult:Reducedp-VEGFR-2expressioninadose-dependentmanner.CellCycleAnalysis[1]CellLine:HT-29cells1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:8.51μMIncubationTime:24hResult:CausedcellgrowtharrestatG2/MbasedonaccumulationofDNAcontentinHT-29cells.ApoptosisAnalysis[1]CellLine:HT-29cellsConcentration:8.51μMIncubationTime:24hResult:ElevatedapoptoticgeneBAXexpressionandsuppressedanti-apoptoticgeneBcl-2expression.Elevatedtotalapoptosispercentage.REFERENCES[1].AbdEl-HaleemAH,etal.Furan-andFuropyrimidine-BasedDerivatives:Synthesis,VEGFR-2Inhibition,andInVitroCytotoxicity.ACSMedChemLett.2024Nov25;15(12):2150-2157.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;