Erdafitinib-JNJ-42756493-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEErdafitinibCat.No.:HY-18708CASNo.:1346242-81-6Synonyms:JNJ-42756493分?式:C??H??N?O?分?量:446.54作?靶點(diǎn):FGFR;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis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:62.5mg/mL(139.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2394mL11.1972mL22.3944mL5mM0.4479mL2.2394mL4.4789mL10mM0.2239mL1.1197mL2.2394mL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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.66mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.66mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.33mg/mL(5.22mM);Clearsolution4.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.75mg/mL(6.16mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(6.16mM);ClearsolutionBIOLOGICALACTIVITY?物活性Erdafitinib(JNJ-42756493)有效的有?服活性的FGFR家族抑制劑；抑制FGFR1-4活性的IC50分別為1.2,2.5,3.0和5.7nM。IC50&TargetFGFR1FGFR2FGFR3FGFR41.2nM(IC50)2.5nM(IC50)3.0nM(IC50)5.7nM(IC50)體外研究Erdafitinib(JNJ-42756493)inhibitsthetyrosinekinaseactivitiesofFGFR1-4intime-resolvedfluorescenceassayswithIC50valuesof1.2,2.5,3.0and5.7nM,respectively.ThecloselyrelatedVEGFR2kinaseislesspotentlyinhibited(30-foldlesspotentcomparedtoFGFR1)byerdafitinib,withanIC50valueof36.8nM.ErdafitinibbindsFGFR1,3,4,and2withKdvaluesof0.24,1.1,1.4and2.2nM,respectively.TheKdvalueforVEGFR2ishigherat6.6nM.ErdafitinibinhibitsproliferationofFGFR1,3,and4expressingcellswithIC50valuesof22.1,13.2,and25nM,respectively[1].體內(nèi)研究Inxenograftsfromhumantumorcelllinesorpatient-derivedtumortissuewithactivatingFGFRalterations,Erdafitinibadministrationresultsinpotentanddose-dependentantitumoractivityaccompaniedbypharmacodynamicmodulationofphospho-FGFRandphospho-ERKintumors[1].PROTOCOLCellAssay[1]ErdafitinibisdissolvedinDMSO.KATOIII,RT-112,A-204,RT-4,DMS-114,A-427andMDA-MB-453cellsaretreatedwitherdafitinib(from10μMto0.01nMin2%DMSO,finalconcentration).Following4-dayincubation,cellviabilityisdeterminedusingMTTreagent.Theopticaldensityisdeterminedat540nm[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:MicebearingSNU-16humangastriccarcinoma(FGFR2amplified)xenografttumorsaredosedorallyAdministration[1]with0,3,10or30mg/kgErdafitinib.Tumortissueandmouseplasma(3micepertimepoint)areharvestedat0.5,1,3,7,16and24hpost-dosing[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CancerDiscov.2019Dec;9(12):1686-1695.?NatCommun.2022Aug4;13(1):4534.?MolPharmacol.April5,2022.?ChemResToxicol.2021Jun30.?JPharmBiomedAnal.2022May30;214:114731.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PereraTP,etal.DiscoveryandpharmacologicalcharacterizationofJNJ-42756493(erdafitinib),afunctionallyselectivesmallmoleculeFGFRfamilyinhibitor.MolCancerTher.2017Mar24.pii:molcanther.0589.2016.McePdfHeightCautio