Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZanubrutinibCat.No.:HY-101474ACASNo.:1691249-45-2Synonyms:BGB-3111分?式:C??H??N?O?分?量:471.55作?靶點:Btk作?通路: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:200mg/mL(424.13mM;Needultrasonic)Ethanol:<1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1207mL10.6033mL21.2067mL5mM0.4241mL2.1207mL4.2413mL10mM0.2121mL1.0603mL2.1207mL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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.41mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.41mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.41mM);ClearsolutionBIOLOGICALACTIVITY?物活性Zanubrutinib(BGB-3111)?個選擇性的Brutontyrosinekinase(Btk)抑制劑。IC50&TargetBTK[1]體外研究Zanubrutinib(BGB-3111)isaselectiveBrutontyrosinekinase(BTK)inhibitor.Inbothbiochemicalandcellularassays,ZanubrutinibdemonstratesnanomolarBTKinhibitionactivity.InseveralMCLandDLBCLcelllines,ZanubrutinibinhibitsBCRaggregation-triggeredBTKautophosphorylation,blocksdownstreamPLC-γ2signaling,andpotentlyinhibitscellproliferation.IncomparisonwithPCI-32765,Zanubrutinibshowsmuchmorerestrictedoff-targetactivitiesagainstapanelofkinases,includingITK[1].體內研究Zanubrutinib(BGB-3111)inducesdose-dependentanti-tumoreffectsagainstREC-1MCLxenograftsengraftedeithersubcutaneouslyorsystemicallyviatailveininjectioninmice.Inthesubcutaneousxenografts,Zanubrutinibat2.5mg/kgBIDshowssimilaractivityasPCI-32765at50mg/kgQD.Inthesystemicmodel,themediansurvivalofZanubrutinib25mg/kgBIDgroupissignificantlylongerthanthoseofbothPCI-3276550mg/kgQDandBIDgroups.InanABC-subtypeDLBCL(TMD-8)subcutaneousxenograftmodel,Zanubrutinibalsodemonstratesbetteranti-tumoractivitythanPCI-32765.Preliminary14-daytoxicitystudyinratsshowsthatZanubrutinibisverywelltoleratedandmaximaltoleratedose(MTD)isnotreachedwhenitisdosedupto250mg/kg/day[1].戶使?本產(chǎn)品發(fā)表的科研?獻?JMedChem.2021Oct21.?Antioxidants(Basel).2021,10(12),1936.?Pharmaceutics.2022,14(10),1994.?ThrombHaemost.2019Mar;119(3):397-406.?LudwigMaximilianUniversityofMunich.2021May.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NaLi,etal.Abstract2597:BGB-3111isanovelandhighlyselectiveBruton'styrosinekinase(BTK)inhibitor.CancerRes2015;75(15Suppl):Abstractnr2597.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidate