EGFR-IN-7-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEGFR-IN-7Cat.No.:HY-128862CASNo.:2267329-76-8分?式:C??H??BrN?O?P分?量:694.6作?靶點(diǎn):EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:5mg/mL(7.20mM;ultrasonicandwarmingandadjustpHto5with0.1MHCLandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4397mL7.1984mL14.3968mL5mM0.2879mL1.4397mL2.8794mL10mM---------請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.25mg/mL(1.80mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(1.80mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(1.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性EGFR-IN-7?種有效的選擇性EGFR激酶抑制劑，具有?服活性。EGFR-IN-7對(duì)EGFR(WT)和EGFR(突變體C797S/T790M/L858R)具有抑制作?，IC50值分別為7.92nM和0.218nM。EGFR-IN-7可?于各種癌癥的研究。IC50&TargetEGFR(WT)EGFR(C797S/T790M/L858R)7.92nM(IC50)0.218nM(IC50)體外研究EGFR-IN-7(compound34)(10mM)hasastronginhibitoryeffectontheenzymaticactivityofEGFR(WT),EGFR(Δ19del/T790M/C797S)andEGFR(C797S/T790M/L858R)withIC50valuesof7.92nM,0.218nMand0.16nM,respectively[1].EGFR-IN-7(1mM)hasexcellentselectivityforEGFR(WT)inA431cellswithanIC50valueof154nM[1].EGFR-IN-7(10μM-0.508nM)hasagoodinhibitoryeffectoncellsoftheBa/F3(EGFRΔ19del/T790M/C797S)triplemutantwithanIC50valueof22nM[1].EGFR-IN-7(10μMor100μM)hasinhibitionofphosphorylationactivityofpEGFRBa/F3(EGFRΔ19del/T790M/C797S)cellswithanIC50valueof19nM[1].CellProliferationAssay[1]CellLine:A431cells;Ba/F3(EGFRΔ19del/T790M/C797S)suspensioncellsConcentration:1mM;10μM-0.508nMIncubationTime:3daysResult:Inhibitedproliferationincells.體內(nèi)研究EGFR-IN-7(compound34;5-45mg/kg;p.o.;daily;for13days)showspotentanti-tumoractivityinasubcutaneouslyimplantedBa/F3(Δ19del/T790M/C797S)-derivedxenograft(CDX)BALB/cnudemouseresistancemodel[1].EGFR-IN-7(25and50mg/kg;p.o.;daily,for3weeks)hasasignificantinhibitoryeffectontumorgrowthinthemousesubcutaneousxenograftPC-9(Δ19del)model[1].AnimalModel:Ba/F3(Δ19del/T790M/C797S)-derivedxenograft(CDX)BALB/cnudemice(female,6-8weeks,18-22g)[1]Dosage:5,15,45mg/kg2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAdministration:Oraladministration,daily,for13daysResult:Significantlyincreasedthehalf-life,theamountofexposureinplasmaandtissues,hadgoodpharmacokineticeffectsinmice.AnimalModel:SubcutaneousxenograftPC-9(Δ19del)model[1]Dosage:0-9days:50mg/kg,10-21days:25mg/kgAdministration:Oraladministration,onceaday,3weeksResult:Hadasignificantinhibitoryeffectontumorgrowth,hadatumor-reducingeffectandshowedgoodantitumorefficacy.REFERENCES[1].LingWY,et,al.ProstaglandinE2suppressesbacterialkillinginalveolarmacrophagesbyinhibitingNADPHoxidase.WO2019015655A1.McePdfHeightCaution:Producthasno