BAY-1816032-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAY-1816032Cat.No.:HY-103020CASNo.:1891087-61-8分⼦式:C₂₇H₂₄F₂N₆O₄分⼦量:534.51作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(46.77mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8709mL9.3544mL18.7087mL5mM0.3742mL1.8709mL3.7417mL10mM0.1871mL0.9354mL1.8709mL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>>90%cornoilSolubility:≥2.5mg/mL(4.68mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性BAY-1816032有效，有⼝服活性的苯并咪唑出芽抑制解除同物蛋⽩1激酶(BUB1(buddinguninhibitedbybenzimidazoles1)kinase)抑制剂，IC50值⼩于7nM。IC50&TargetIC50:7nM(BUB1)[1]体外研究BAY-1816032inhibitsBUB1enzymaticactivitywithanIC50of7nM,showsslowdissociationkineticsresultinginalongtargetresidencetimeof87min,andanexcellentselectivityonapanelof395kinases.MechanisticallyBAY-1816032abrogatesnocodazole-inducedThr-120phosphorylationofthemajorBUB1targetproteinhistoneH2AinHeLacellswithanIC50of29nM,inducedlaggingchromosomesandmitoticdelay.Persistentlaggingchromosomesandmissegregationareobserveduponcombinationwithlowconcentrationsofpaclitaxel.SingleagentBAY-1816032inhibitsproliferationofvarioustumorcelllineswithamedianIC50of1.4μManddemonstratessynergyoradditivitywithpaclitaxelordocetaxelinalmostallcelllinesevaluated(minimalcombinationindex0.3)[1].体内研究IntumorxenograftstudiesBAY1816032onlymarginallyinhibitstumorgrowthassingleagentuponoraladministration,however,uponcombinationwithpaclitaxelordocetaxelastrongandstatisticallysignificantreductionoftumorsizeascomparedtotherespectivemonotherapyisobserved[1].户使⽤本产品发表的科研⽂献•Cell.2019Aug22;178(5):1132-1144.e10.•SciAdv.2022Jan21;8(3):eabk0114.•JProteomeRes.2021Jun4.•bioRxiv.2021Feb5.•bioRxiv.2020Jun.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SiemeisterG,etal.BAY1816032,anovelBUB1kinaseinhibitorwithpotentantitumoractivity[abstract].In:ProceedingsoftheAmericanAssociationforCancerResearchAnnualMeeting2017;2017Apr1-5;Ishington,DC.Philadelphia(PA):AACR;CancerReMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic