Mobocertinib-mesylate-TAK-788-mesylate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMobocertinibmesylateCat.No.:HY-135815BCASNo.:2389149-85-1Synonyms:TAK-788mesylate;AP32788mesylate分⼦式:C₃₃H₄₃N₇O₇S分⼦量:681.8作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Mobocertinib(TAK-788)mesylate⼀种⼝服有效并且不可逆的EGFR/HER2抑制剂。Mobocertinibmesylate能选择性地(相较于野⽣型EGFR)抑制含有EGFRex20ins的致癌突变体。Mobocertinibmesylate可⽤于NSCLC的研究。IC50&TargetHER2EGFRexon20insertionEGFR(WT)体外研究Mobocertinibmesylate(1.5nM-10μM;7days)inhibitsLU0387(NPH)cellswithIC50of21nM[1].Mobocertinibmesylate(2h)potentlyinhibitsEGFRwithcommonactivatingmutations(HCC827(D),HCC4011(L))orwithaT790Mmutation(H1975(LT))morepotentlythanWTEGFR(A431(WT))[1].Mobocertinibmesylate(0.1nM-1μM;6h)inhibitspEGFRandpERK1/2inCUTO14(ASV)cells[1].Mobocertinibmesylate(0.3nM-1μM;6h)inhibitsEGFRanddownstreamsignaling[1].Mobocertinibmesylate(0.01,0.1and1μM;6h)inhibitsHER2signalinginH1781(HER2Exon20G776>VC),Ba/F3(HER2exon20YVMA)cells[2].CellViabilityAssay[1]CellLine:LU0387(NPH)cellsConcentration:1.5nM-10μMIncubationTime:7daysResult:ShowedgoodinhibitionactivityforLU0387(NPH)cellswithIC50of21nM.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellViabilityAssay[1]CellLine:A431(WT),HCC827(D),HCC4011(L),H1975(LT)cellsConcentration:IncubationTime:2hResult:InhibitedEGFRwithcommonactivatingmutationsofHCC827(D),HCC4011(L)cellsandT790MmutationofH1975(LT)withIC50sof4,1.3and9.8nMrespectively,whichmorepotentlythanWTEGFR(A431(WT);IC50of35nM).WesternBlotAnalysis[1]CellLine:CUTO14(ASV)cellsConcentration:0.1nM-1μMIncubationTime:6hResult:RobustlyinhibitedEGFRsignaling,reaching80%and100%inhibitionofphosphorylatedEGFR(pEGFR)atconcentrationsof100nMand1μM,respectively.WesternBlotAnalysis[1]CellLine:HCC827(D),HCC4011(L),H1975(LT)cellsConcentration:0.3nM-1μMIncubationTime:6hResult:PotentlyinhibitedEGFRanddownstreamsignalinginHCC827(D),HCC4011(L)andH1975(LT)cells.WesternBlotAnalysis[2]CellLine:H1781(HER2Exon20G776>VC),Ba/F3(HER2exon20YVMA)cellsConcentration:0.01,0.1and1μMIncubationTime:6hResult:InhibitedHER2signalinginH1781andBa/F3-HER2exon20YVMAmutantcellsat0.1μMwithsignificantlydecreasedphosphorylationsofHER2,AKT,andERK1/2inadose-dependentmanner.体内研究Mobocertinibmesylate(3,10,30mg/kg;p.o.;oncedailyfor20days)significantlyinducestumorgrowthinhibition[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Animalmodel:FemaleAthymicNude-Foxn1numice(humanNSCLCH1975LTtumormodel)[1].Dosage:3,10,30mg/kgAdministration:Oral;oncedailyfor20days.Result:Decreasedthemeantumorvolumeby44%and92%whenat3mg/kgand10mg/kg,respectively,relativetothetumorsizeofvehiclegroup.Induceda76%tumorregressionrelativetothepretreatmenttumorsizeat30mg/kg.户使⽤本产品发表的科研⽂献•Cells.2021,10(12),3561.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GonzalvezF,etal.Mobocertinib(TAK-788):ATargetedInhibitorofEGFRExon20InsertionMutantsinNon-SmallCellLungCancer.CancerDiscov.2021Jul;11(7):1672-1687.[2].HanH,etal.TargetingHER2Exon20Insertion-MutantLungAdenocarcinomawithaNovelTyrosineKinaseInhibitorMobocertinib.CancerRes.2021Oct15;81(20):5311-5324.McePdfHeightCaution:Product