Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEElzovantinibCat.No.:HY-111787CASNo.:2271119-26-5Synonyms:TPX-0022;CSF1R-IN-2分?式:C??H??FN?O?分?量:409.42作?靶點:Src;c-Met/HGFR;c-Fms作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:25mg/mL(61.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4425mL12.2124mL24.4248mL5mM0.4885mL2.4425mL4.8850mL10mM0.2442mL1.2212mL2.4425mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.08mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性Elzovantinib(TPX-0022)SRC，MET和c-FMS的?服有效抑制劑,其對SRC，MET和c-FMS的IC50值分別為0.12nM，0.14nM和0.76nM。IC50&TargetIC50:0.12nM(SRC),0.14nM(MET),0.76nM(c-FMS)[1].體外研究Elzovantinib(TPX-0022)causesthesuppressionofMETautophosphorylationaswellasthedownstreamSTAT3,ERKandAKTphosphorylationatIC50valuesofaround1-3nMinSNU-5andMKN-45celllines[1].體內研究Elzovantinib(TPX-0022;p.o.,BID,13days)treatmentresultsinan85%tumorregressionandnobodyweightlossisobservedafter21daystreatmentinmice[1].Elzovantinib(p.o.,BID,10days)demonstratestheabilitytoinhibittumorgrowthat44%and67%atthedoseof5mg/kg,BIDand15mg/kg,BID,respectivelyinSCID/Beigemice[1].ElzovantinibinhibitsMETactivityinMKN-45tumorsfollowingoraladministrationinmice[1].AnimalModel:MicebearingLU2503tumorspatientderivedxenograft(PDX)NSCLCmodel[1].Dosage:15mg/kg.Administration:PO,BID(twicedaily)for13days.Result:Resultedinan85%tumorregressionandnobodyweightlosswasobservedafter21daystreatment.AnimalModel:SCID/BeigemicebearingBa/F3ETV6-CSF1Rtumorswithaveragetumorsizeof~180mm3[1].Dosage:5and15mg/kg.Administration:PO,BID(twicedaily)for10days.Result:Demonstratedtheabilitytoinhibittumorgrowthat44%and67%atthedoseof5mg/kg,BIDand15mg/kg,BID,respectively.REFERENCES[1].WO2019023417A1.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicatio