Vecabrutinib-SNS-062-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVecabrutinibCat.No.:HY-109078CASNo.:1510829-06-7Synonyms:SNS-062分⼦式:C₂₂H₂₄ClF₄N₇O₂分⼦量:529.92作⽤靶点:Btk;Itk作⽤通路: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(235.88mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8871mL9.4354mL18.8708mL5mM0.3774mL1.8871mL3.7742mL10mM0.1887mL0.9435mL1.8871mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.93mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.93mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.93mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.72mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.72mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Vecabrutinib(SNS-062)⼀种有效的，⾮共价的BTK和ITK抑制剂，Kd值分别为0.3nM和2.2nM。Vecabrutinib对ITK的IC50值为24nM。IC50&TargetIC50:24nM(ITK)[2]Kd:0.3nM(BTK),2.2nM(ITK)[1]体外研究VecabrutinibinhibitspBTKinhumanwholebloodwithanaverageIC50of50nM.VecabrutinibinhibitsWTandC481SBTKwithsimilarIC50s(pBTKIC50s:WTBTK2.9nM,C481SBTK4.4nM)[1].Inarecombinantkinaseassay,IC50sofVecabrutinibagainstWTBTKandC481SBTKare4.6nMand1.1nM.VecabrutinibretainsactivityagainstthemutatedBTKvariant.VecabrutinibissixtimesmorepotentthanPCI-32765andgreaterthan640timesmorepotentthanacalabrutinibagainstC481SBTK.Vecabrutinibdemonstratesdose-dependentinhibitionofBTKinprimarypatientCLLcellscomparabletoPCI-32765viaimmunoblotforBTKphosphorylation.VecabrutinibdecreasesviabilityofprimaryCLLcellsinthepresenceofHS5stromalprotectionby5.5%[2].体内研究Vecabrutinibhasgoodoralbioavailabilityinratanddog(%F≥40%)andaterminalhalf-lifeof5to6hours.VecabrutinibiswelltoleratedwithcontinuousdruglevelsandatexposuresmuchgreaterthanthoseachievedforPCI-32765[1].户使⽤本产品发表的科研⽂献•ProcNatlAcadSciUSA.2022Oct25;119(43):e2207280119.•JCIInsight.2019Jun20;4(12).pii:127566.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MinkeE.Binnerts,etal.AbstractC186:SNS-062isapotentnoncovalentBTKinhibitorwithcomparableactivityagainstwildtypeBTKandBTKwithanacquiredresistancemutation.MolecularCancerTherapeutics.December2015Volume14,Issue12Supplement2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].CatherineA.Fabian,etal.Abstract1207:SNS-062demonstratesefficacyinchroniclymphocyticleukemiainvitroandinhibitsC481SmutatedBrutontyrosinekinase.CancerResearchJuly2017Volume77,Issue13SupplementMcePdfHeightCaution:Producthasnotbeenfu