BLU-945-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBLU-945Cat.No.:HY-144680CASNo.:2660250-10-0分⼦式:C₂₈H₃₇FN₆O₃S分⼦量:556.7作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:125mg/mL(224.54mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7963mL8.9815mL17.9630mL5mM0.3593mL1.7963mL3.5926mL10mM0.1796mL0.8981mL1.7963mL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(protectfromlight)。-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%salineSolubility:2.08mg/mL(3.74mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.74mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性BLU-945⼀种强效、⾼选择性、可逆的表⽪⽣长因⼦受体酪氨酸激酶抑制剂(TKIs)，具有⼝服活性。BLU-945可有效抑制具有L858R和/或外显⼦19缺失突变、T790M突变和C797S突变的EGFR。BLU-945可⽤于肺癌包括⾮⼩细胞肺癌（NSCLC）的研究。体外研究BLU-945hasinhibitoryactivityagainsttheEGFRm/T790MdoubleandEGFRm/T790M/C797StriplemutantswithIC50valuerangefrom1.2-4.4nM[2].BLU-945(0-10mM,4h)inhibitEGFRphosphorylationintheEGFRL858R/T790M/C797S,andEGFRex19del/T790M/C797Smutantcelllines[2].体内研究BLU-945(oral,0-100mg/kg;bid)demonstratespotent,robustEGFRpathwayinhibitionandanti-tumoractivityintriple-mutantosimertinib-resistantBa/F3CDXandPDCXmodels[2].AnimalModel:triple-mutantosimertinib-resistantBa/F3CDXandPDCXmodels[2]Dosage:0-100mg/kgAdministration:oral,twicedailyResult:Showedsignificanttumorregressioninanosimertinib-resistantEGFRex19del/T790M/C797SPDCX.REFERENCES[1].SunMinLim,etal.BLU-945,afourth-generation,potentandhighlyselectiveepidermalgrowthfactorreceptortyrosinekinaseinhibitorwithintracranialactivity,demonstratesrobustinvivoanti-tumoractivityinmodelsofosimertinib-resistantnon-sma[2].MeredithSEno,etal.DiscoveryofBLU-945,aReversible,Potent,andWild-Type-SparingNext-GenerationEGFRMutantInhibitorforTreatment-ResistantNon-Small-CellLungCancer.JMedChem.2022Jul28;65(14):9662-9677.[3].ElaineShum.etal.Aphase1/2studyofBLU-945inpatientswithcommonactivatingEGFRmutantnon-smallcelllungcancer(NSCLC)(SYMPHONYtrial-in-progress)[4].JohnEmmersonCampbell,etal.Inhibitorsofmutantformsofegfr.PatentWO2021133809A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical