FIIN-3-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFIIN-3Cat.No.:HY-18603CASNo.:1637735-84-2分⼦式:C₃₄H₃₆Cl₂N₈O₄分⼦量:691.61作⽤靶点:EGFR;FGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:10mg/mL(14.46mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4459mL7.2295mL14.4590mL5mM0.2892mL1.4459mL2.8918mL10mM0.1446mL0.7230mL1.4459mL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。-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:≥2.5mg/mL(3.61mM);Clearsolution1/2MasterofBioactiveMolecules—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:2.5mg/mL(3.61mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.61mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FIIN-3FGFR的不可逆抑制剂，对FGFR1，FGFR2，FGFR3和FGFR4的IC50值分别为13.1，21，31.4和35.3nM。IC50&TargetFGFR1FGFR2FGFR3FGFR413.1nM(IC50)21nM(IC50)31.4nM(IC50)35.3nM(IC50)体外研究FIIN-3potentlyinhibitsbothWTFGFRs(EC50inthe1-to41-nMrange)andthegatekeepermutantofFGFR2(EC50of64nM).FIIN-3alsostronglyinhibitsEGFR,withanEC50of43nM.FIIN-3showsgoodpotencyagainstgatekeepermutantV564F;FIIN-3alsoispotentagainstthegatekeeper-plus-1mutantE565K;FIIN-3alsodisplaysantiproliferativeactivity(withanEC50of135nM)againstBa/F3cellstransformedbytheEGFRvIIIfusionprotein,whichhasaWTEGFRkinasedomain.FIIN-3showsevenbetteractivityagainstEGFRmutantL858R(EC50of17nM)andmoderateactivity,displayinganEC50of231nM,againsttheEGFRmutantL858R/T790Mmutant.InWTFGFR2Ba/F3cells,FIIN-3completelyinhibitstheFGFR2autophosphorylationonTyr656/657atconcentrationsaslowas3nM.InFGFR2V564MBa/F3cells,FIIN-3iscapableofinhibitingtheFGFR2mutantV564Mautophosphorylationwithpartialinhibitionat100nMandcompleteinhibitionobservedat300nM[1].PROTOCOLCellAssay[1]TEL-FGFR2–transformedBa/F3cellsareseededina96-wellplateandaretreatedwitheachconcentrationofFIIN-3.After72hthecellsareassessedbyMTStetrazoliumassay[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].TanLetal.Developmentofcovalentinhibitorsthatcanovercomeresistancetofirst-generationFGFRkinaseinhibitors.ProcNatlAcadSciUSA,2014Nov11,111(45):E4869-77McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica