Elzovantinib-TPX-0022-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEElzovantinibCat.No.:HY-111787CASNo.:2271119-26-5Synonyms:TPX-0022;CSF1R-IN-2分⼦式:C₂₀H₂₀FN₇O₂分⼦量:409.42作⽤靶点:Src;c-Met/HGFR;c-Fms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:25mg/mL(61.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4425mL12.2124mL24.4248mL5mM0.4885mL2.4425mL4.8850mL10mM0.2442mL1.2212mL2.4425mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Elzovantinib(TPX-0022)SRC，MET和c-FMS的⼝服有效抑制剂,其对SRC，MET和c-FMS的IC50值分别为0.12nM，0.14nM和0.76nM。IC50&TargetIC50:0.12nM(SRC),0.14nM(MET),0.76nM(c-FMS)[1].体外研究Elzovantinib(TPX-0022)causesthesuppressionofMETautophosphorylationaswellasthedownstreamSTAT3,ERKandAKTphosphorylationatIC50valuesofaround1-3nMinSNU-5andMKN-45celllines[1].体内研究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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicatio