JNJ-38877618-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJNJ-38877618Cat.No.:HY-111050CASNo.:943540-74-7分⼦式:C₂₀H₁₂F₂N₆分⼦量:374.35作⽤靶点:c-Met/HGFR作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:5mg/mL(13.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6713mL13.3565mL26.7130mL5mM0.5343mL2.6713mL5.3426mL10mM0.2671mL1.3356mL2.6713mL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:≥0.5mg/mL(1.34mM);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:≥0.5mg/mL(1.34mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥0.5mg/mL(1.34mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JNJ-38877618⼀种有效的，⾼选择性的，⼝服可⽤的(Met)激酶抑制剂，对于野⽣型和突变体的IC50值分别为2和3nM。IC50&TargetIC50:2nM(wtMet),2nM(mutantMet)[1]体外研究OMO-1(formerlyJNJ-38877618),isapotent,highlyselective,orallybioavailableMetkinaseinhibitorwithnMbindingaffinity(Kd=1.4nM)andenzymeinhibitoryactivityagainstwtandM1268TmutantMet(2and3nMIC50).Metinhibitoryeffectsareassessedinproliferation,colonyformationandmotilityassays.JNJ-38877618displaysnMpotencyagainstMetAmpl/mutantandtherapyresistantmodels[1].体内研究JNJ-38877618inducescompleteinhibitionoftumorgrowthin3models:theSNU5Metampgastric,U87-MGHGFautocrineglioblastomaandHs746TMetexon14skippingmutantgastriccancer.JNJ-38877618inducesregressionoflargeMetamplifiedEBC-1SqNSCLCwhereJNJ-38877618leadstodose-andtime-dependentinhibitionofMetkinaseactivation,withthedurationoftargetshutdownconsiderablyexceedingplasmaexposuretimes.CombinationtreatmentsarewelltoleratedandimprovedEGFRtargetedtherapy[1].REFERENCES[1].LiboubanM,etal.OMO-1,apotent,highlyselective,orallybioavailable,Metkinaseinhibitorwithafavorablepreclinicaltoxicityprofile,showsbothmonotherapyactivity,againstMetpathway-driventumors,andEGFRTKIcombinationactivityinacquireMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo