Rezivertinib-BPI-7711-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERezivertinibCat.No.:HY-109189CASNo.:1835667-12-3Synonyms:BPI-7711分⼦式:C₂₇H₃₀N₆O₃分⼦量:486.57作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(256.90mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0552mL10.2760mL20.5520mL5mM0.4110mL2.0552mL4.1104mL10mM0.2055mL1.0276mL2.0552mL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(4.27mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.27mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Rezivertinib(BPI-7711)⼀种⼝服有效，⾼选择性和不可逆的第三代EGFR酪氨酸激酶抑制剂(TKI)。Rezivertinib对常见的激活EGFR和抗性T790M突变具有⾼效⼒。Rezivertinib具有出⾊的透过中枢神经系统(CNS)能⼒，并具有抗肿瘤活性。IC50&TargetEGFR体外研究Rezivertinib(BPI-7711)selectivelyinhibitscellularproliferationofEGFRmutationsincelllines:GI5013.3nM(PC9,del19),6.8nM(HCC827,L858R),22nM(NCI-H1975,del19/T790M)and>1000nM(A431,EGFRWT)[1].体内研究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