EG00229-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEG00229Cat.No.:HY-10799CASNo.:1210945-69-9分?式:C??H??F?N?O?S?分?量:611.6作?靶點:ComplementSystem作?通路:Immunology/Inflammation儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:≥41.4mg/mL(67.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6351mL8.1753mL16.3506mL5mM0.3270mL1.6351mL3.2701mL10mM0.1635mL0.8175mL1.6351mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.09mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.09mM);ClearsolutionBIOLOGICALACTIVITY?物活性EG00229?種神經(jīng)纖維蛋?1受體(NRP1)拮抗劑。EG00229選擇性抑制VEGF-A與NRP1b1域的結(jié)合，IC50為3μM，但對VEGFA與VEGFR-1和VEGFR-2的結(jié)合沒有響。IC50&TargetIC50:8μM(125I-VEGF-AbindingtoPAE/NRP1);3μM(bt-VEGF-AbindingtopurifiedNRP1b1domain)[1].體外研究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.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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