BAY-1816032-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBAY-1816032Cat.No.:HY-103020CASNo.:1891087-61-8分?式:C??H??F?N?O?分?量:534.51作?靶點(diǎn):Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(46.77mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8709mL9.3544mL18.7087mL5mM0.3742mL1.8709mL3.7417mL10mM0.1871mL0.9354mL1.8709mL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(fù)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(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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>>90%cornoilSolubility:≥2.5mg/mL(4.68mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性BAY-1816032有效，有?服活性的苯并咪唑出芽抑制解除同物蛋?1激酶(BUB1(buddinguninhibitedbybenzimidazoles1)kinase)抑制劑，IC50值?于7nM。IC50&TargetIC50:7nM(BUB1)[1]體外研究BAY-1816032inhibitsBUB1enzymaticactivitywithanIC50of7nM,showsslowdissociationkineticsresultinginalongtargetresidencetimeof87min,andanexcellentselectivityonapanelof395kinases.MechanisticallyBAY-1816032abrogatesnocodazole-inducedThr-120phosphorylationofthemajorBUB1targetproteinhistoneH2AinHeLacellswithanIC50of29nM,inducedlaggingchromosomesandmitoticdelay.Persistentlaggingchromosomesandmissegregationareobserveduponcombinationwithlowconcentrationsofpaclitaxel.SingleagentBAY-1816032inhibitsproliferationofvarioustumorcelllineswithamedianIC50of1.4μManddemonstratessynergyoradditivitywithpaclitaxelordocetaxelinalmostallcelllinesevaluated(minimalcombinationindex0.3)[1].體內(nèi)研究IntumorxenograftstudiesBAY1816032onlymarginallyinhibitstumorgrowthassingleagentuponoraladministration,however,uponcombinationwithpaclitaxelordocetaxelastrongandstatisticallysignificantreductionoftumorsizeascomparedtotherespectivemonotherapyisobserved[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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