EG00229-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEG00229Cat.No.:HY-10799CASNo.:1210945-69-9分⼦式:C₁₉H₂₀F₃N₇O₇S₃分⼦量:611.6作⽤靶点:ComplementSystem作⽤通路:Immunology/Inflammation储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥41.4mg/mL(67.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6351mL8.1753mL16.3506mL5mM0.3270mL1.6351mL3.2701mL10mM0.1635mL0.8175mL1.6351mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.09mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.09mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性EG00229⼀种神经纤维蛋⽩1受体(NRP1)拮抗剂。EG00229选择性抑制VEGF-A与NRP1b1域的结合，IC50为3μM，但对VEGFA与VEGFR-1和VEGFR-2的结合没有响。IC50&TargetIC50:8μM(125I-VEGF-AbindingtoPAE/NRP1);3μM(bt-VEGF-AbindingtopurifiedNRP1b1domain)[1].体外研究EG00229(Compound2;0-100μM;48hours;A549cells)treatmentcausesasignificantreductionincellviabilityovera48hoursincubation[1].EG00229(Compound2)demonstratesinhibitionofVEGF-AbindingtoNRP1andattenuatesVEGFR2phosphorylationinendothelialcells.InhibitionofmigrationofendothelialcellsisalsoobservedinHUVECs[1].EG00229(Compound2)selectivelyinhibitsradiolabeled125I-VEGF-Abindingtoporcineaorticendothelial(PAE)/NRP1,butnotVEGFR2-expressingcells,withanIC50of8μM.EG00229alsoinhibitsVEGF-AbindingtolungcarcinomaA549andprostatecarcinomaDU145cells,whichexpressNRP1,butnotVEGFR1andVEGFR2,withsimilarpotency.BindingofVEGF-Atohumanumbilicalveinendothelialcells(HUVECs),whichexpressVEGFR2,VEGFR1,andNRP1,isalsoinhibitedbyEG00229withanIC50of23μM[1].CellViabilityAssay[1]CellLine:A549cellsConcentration:0µM,10μM,30μM,100μMIncubationTime:48hoursResult:Causedasignificantreductionincellviability.体内研究EG00229(0-10mg/kg;intraperitonealinjection;threetimesperweek;for4weeks;NSGmice)treatmentsubstantiallyreducestumorgrowthandvisiblevascularization[2].AnimalModel:6-weekoldfemaleNODscidIL2receptorgammachainknockoutmice(NSGmice)withECScells[2]Dosage:0mg/kg,10mg/kgAdministration:Intraperitonealinjection;threetimesperweek;for4weeksResult:Reducestumorgrowthandvisiblevascularization.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•EBioMedicine.2019May;43:525-536.•EBioMedicine.2019May;43:525-536.•BiochemPharmacol.2022May;199:115030.•JCancer.2021Aug24;12(20):6105-6117.•JCancer.2021Aug.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JarvisA,etal.Smallmoleculeinhibitorsoftheneuropilin-1vascularendothelialgrowthfactorA(VEGF-A)interaction.JMedChem.2010Mar11;53(5):2215-26.[2].GrunD,etal.VEGF-Aactsvianeuropilin-1toenhanceepidermalcancerstemcellsurvivalandformationofaggressiveandhighlyvascularizedtumors.Oncogene.2016Aug18;35(33):4379-87.McePdfHeightCaution:Producthas