EGFR-IN-1-TFA-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEEGFR-IN-1TFACat.No.:HY-19617B分?式:C??H??F?N?O?分?量:628.6作?靶點:EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(397.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5908mL7.9542mL15.9084mL5mM0.3182mL1.5908mL3.1817mL10mM0.1591mL0.7954mL1.5908mL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，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性EGFR-IN-1TFA?種?服活性不可逆的突變型選擇性L858R/T790MEGFR抑制劑。與野?型EGFR相?，EGFR-IN-1TFA對Gefitinib耐藥的EGFRL858R/T790M有100倍的抑制作?。EGFR-IN-1TFA對H1975細(xì)胞和HCC827細(xì)胞具有較強(qiáng)的抗增殖活性。具有抗腫瘤活性。IC50&TargetEGFRL858R/T790M體外研究EGFR-IN-1TFA(compound24)isanorallyactiveandirreversibleL858R/T790MmutantselectiveEGFRinhibitor.EGFR-IN-1TFApotentlyinhibitsGefitinib-resistantEGFRL858R,T790Mwith100-foldselectivityoverwild-typeEGFR.EGFR-IN-1TFAdisplaysstrongantiproliferativeactivityagainsttheH1975cellsand1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEthefirstlinemutantHCC827cells.Antitumoractivity[1].CellProliferationAssay[1]CellLine:NSCLCcelllinesH1975(T790M/L858R),HCC827(?746-750)Concentration:10μMIncubationTime:72hoursResult:InhibitedH1975nonsmallcelllungcancercelllineandthefirstlinemutantHCC827celllinewithIC50sof4and28nM,respectively.體內(nèi)研究EGFR-IN-1TFA(30mg/kg;p.o.;dailyfor2weeks)displayssignificanttumorgrowthinhibitionwithnoobservedlossinbodyweight[1].EGFR-IN-1TFAevaluatesinatimecoursePDexperimentuponoraldosingat30mg/kg.EGFR-IN-1TFAshowsa>50%inhibitionofphosphorylationofEGFRfor>12h.EGFR-IN-1TFAreachesmaximalconcentrationof0.10μMat2handsystemicexposure(AUC0-inf.)is0.33μM.h[1].REFERENCES[1].WurzRP,etal.Oxopyrido[2,3-d]pyrimidinesasCovalentL858R/T790MMutantSelectiveEpidermalGrowthFactorReceptor(EGFR)Inhibitors.ACSMedChemLett.2015Jul27;6(9):987-92.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl