JNJ-38877618-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJNJ-38877618Cat.No.:HY-111050CASNo.:943540-74-7分?式:C??H??F?N?分?量:374.35作?靶點(diǎn):c-Met/HGFR作?通路: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(13.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6713mL13.3565mL26.7130mL5mM0.5343mL2.6713mL5.3426mL10mM0.2671mL1.3356mL2.6713mL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:≥0.5mg/mL(1.34mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥0.5mg/mL(1.34mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.5mg/mL(1.34mM);ClearsolutionBIOLOGICALACTIVITY?物活性JNJ-38877618?種有效的，?選擇性的，?服可?的(Met)激酶抑制劑，對(duì)于野?型和突變體的IC50值分別為2和3nM。IC50&TargetIC50:2nM(wtMet),2nM(mutantMet)[1]體外研究OMO-1(formerlyJNJ-38877618),isapotent,highlyselective,orallybioavailableMetkinaseinhibitorwithnMbindingaffinity(Kd=1.4nM)andenzymeinhibitoryactivityagainstwtandM1268TmutantMet(2and3nMIC50).Metinhibitoryeffectsareassessedinproliferation,colonyformationandmotilityassays.JNJ-38877618displaysnMpotencyagainstMetAmpl/mutantandtherapyresistantmodels[1].體內(nèi)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