Rezivertinib-BPI-7711-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERezivertinibCat.No.:HY-109189CASNo.:1835667-12-3Synonyms:BPI-7711分?式:C??H??N?O?分?量:486.57作?靶點:EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(256.90mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0552mL10.2760mL20.5520mL5mM0.4110mL2.0552mL4.1104mL10mM0.2055mL1.0276mL2.0552mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?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(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)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(4.27mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.27mM);ClearsolutionBIOLOGICALACTIVITY?物活性Rezivertinib(BPI-7711)?種?服有效，?選擇性和不可逆的第三代EGFR酪氨酸激酶抑制劑(TKI)。Rezivertinib對常見的激活EGFR和抗性T790M突變具有?效?。Rezivertinib具有出?的透過中樞神經(jīng)系統(tǒng)(CNS)能?，并具有抗腫瘤活性。IC50&TargetEGFR體外研究Rezivertinib(BPI-7711)selectivelyinhibitscellularproliferationofEGFRmutationsincelllines:GI5013.3nM(PC9,del19),6.8nM(HCC827,L858R),22nM(NCI-H1975,del19/T790M)and>1000nM(A431,EGFRWT)[1].體內(nèi)研究Rezivertinib(BPI-7711;6.25-25mg/kg/day;orally;14days)showssignificanttumorregression[2].Rezivertinib(12.5mg/kg/day;orally;14days)survivesanaverageof112%longerinH1975-luchumanNSCLCmicemodel[2].Rezivertinib(50mg/kg/day;orally)hasanti-tumorefficacycorrelatedtoimprovedaverageoverallsurvivaloftheanimalsof115%(28daysvs.13days)[2].REFERENCES[1].MisakoNagasaka,etal.BeyondOsimertinib:TheDevelopmentofThird-GenerationEGFRTyrosineKinaseInhibitorsForAdvancedEGFR+NSCLC.JThoracOncol.2021May;16(5):740-763.[2].VictoriaL.Wilde,etal.PreclinicalevidenceofBPL-7711activityinEgfr-mutantnon-smallcelllungcancer(NSCLC)inorthotopicallyimplantedhumantumorxenograftsinthelungandbrain.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch