EGFR-IN-139-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEGFR-IN-139Cat.No.:HY-170438CASNo.:1574321-31-5分?式:C??H??ClN?O?分?量:476.95作?靶點(diǎn):EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性EGFR-IN-139(compoundPD18)?種EGFR抑制劑，IC50分別為12.88(野?型)，10.84(L858R/T790M)，42.68(L858R/T790M/C797S)nM。EGFR-IN-139對(duì)?度表達(dá)EGFR的A549和H1975癌細(xì)胞系顯?出強(qiáng)烈的抗癌活性。EGFR-IN-139對(duì)癌細(xì)胞具有很強(qiáng)的選擇性。EGFR-IN-139可?于??細(xì)胞肺癌(NSCLC)的研究。體外研究EGFR-IN-139(1μM,2h)inhibitswild-typeEGFRandL858R/T790MEGFRwithinhibitionratesof90-100%and65-75%,respectively[1].EGFR-IN-139(0-100μM,72h)inhibitsA549,H1975,VerocellswithIC50sof28.23,29.46,180.9μM,respectively[1].CellProliferationAssayCellLine:A549,H1975cellsConcentration:0-100μMIncubationTime:72hResult:InhibitedA549,H1975,VerocellswithIC50sof28.23(similartothatofErlotinib(HY-50896)),29.46,180.9μM,.Wasrelativelysafefornormalcells,asitsIC50valueinVerocellswashighercomparedtothoseinA549(SI(IC50ofA549andH1975)versusIC50ofVero)of6.40)andH1975(SIof6.14).1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].TodsapornD,etal.FuropyridineDerivativesasPotentInhibitorsoftheWildType,L858R/T790M,andL858R/T790M/C797SEGFR.JPhysChemB.2024Dec19;128(50):12389-12402.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792/p>