Naquotinib-mesylate-ASP8273-mesylate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENaquotinibmesylateCat.No.:HY-19803CASNo.:1448237-05-5Synonyms:ASP8273(mesylate)分⼦式:C₃₁H₄₆N₈O₆S分⼦量:658.81作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:12.5mg/mL(18.97mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5179mL7.5894mL15.1789mL5mM0.3036mL1.5179mL3.0358mL10mM0.1518mL0.7589mL1.5179mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2mg/mL(3.04mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(3.04mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Naquotinibmesylate(ASP8273mesylate)有⼝服活性，不可逆的EGFR突变体抑制剂；对EGFR突变体和EGFR的IC50值分别为8-33和230nM。IC50&TargetEGFRL858R/T790MEGFRL858REGFRExon19EGFRExon19(IC50)(IC50)deletiondeletion/T790M(IC50)(IC50)EGFR230nM(IC50)体外研究InassaysusingendogenouslyEGFR-dependentcells,NaquotinibinhibitsthegrowthofPC-9(delex19),HCC827(delex19),NCI-H1975(delex19/T790M)andPC-9ER(delex19/T790M)withIC50sof8-33nM[1].NaquotinibselectivelyinhibitsphosphorylationofEGFRanditsdown-streamsignalpathway,ERKandAktfrom10nMinHCC827andNCI-H1975whileinhibitoryeffectsareonlydetectedat1000nMinA431.InNCI-H1650(delex19),NaquotinibinhibitscellgrowthwithanIC50valueof70nMwhileotherEGFR-TKIsareonlypartiallyeffective[2].体内研究OralNaquotinibtreatmentdosedependentlyinducestumorregressioninNCI-H1975(L858R/T790M),HCC827(delex19)andPC-9(delex19)xenograftmodels.DosingschedulesdoesnotaffecttheefficacyofNaquotinib.InanNCI-H1975xenograftmodel,completeregressionoftumorisachievedafter14-daysofNaquotinibtreatment.Completeregressionismaintainedin50%ofmicemorethan85daysaftercessationofNaquotinibtreatment[2].户使⽤本产品发表的科研⽂献•RSCAdv.2019,9(18):10211-10225.•RSCAdv.2019,9,4862-4869•RSocOpenSci.2019Jun5;6(6):190434.•bioRxiv.2020Jun.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SakagamiH,etal.ASP8273,anovelmutant-selectiveirreversibleEGFRinhibitor,inhibitsgrowthofnon-smallcelllungcancer(NSCLC)cellswithEGFRactivatingandT790Mresistancemutations.[abstract].In:Proceedingsofthe105thAnnualMeetingoft[2].KonagaiS,etal.ASP8273selectivelyinhibitsmutantEGFRsignalpathwayandinducestumorshrinkageinEGFRmutatedtumormodels.[abstract].In:Proceedingsofthe106thAnnualMeetingoftheAmericanAssociationforCancerResearch;2015Apr18-22;Ph2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfully