ABBV-744-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEABBV-744Cat.No.:HY-112090CASNo.:2138861-99-9分⼦式:C₂₈H₃₀FN₃O₄分⼦量:491.55作⽤靶点:EpigeneticReaderDomain;HIV作⽤通路:Epigenetics;Anti-infection储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(203.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0344mL10.1719mL20.3438mL5mM0.4069mL2.0344mL4.0688mL10mM0.2034mL1.0172mL2.0344mL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(storedundernitrogen)。-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:≥2.5mg/mL(5.09mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.09mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.09mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2mg/mL(4.07mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(4.07mM);Clearsolution6.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:2.5mg/mL(5.09mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性ABBV-744⼀种⾸创，具有⼝服活性和选择性的BET家族蛋⽩BDII结构域(BDIIdomain)，对BRD2、BRD3、BRD4和BRDT的IC50值为4~18nM。ABBV-744主由CYP3A4代谢，具有类似药物的特性，可⽤于研究其抗肿瘤功效和耐受性[1]。IC50&TargetBRD2(BD2)BRD3(BD2)BRDT(BD2)BRD4(BD2)8nM(IC50)13nM(IC50)18nM(IC50)4nM(IC50)BRD4(BD2)3nM(Kd)体外研究ABBV-744(90nM;0~24h;LNCaPcells)downregulatestheexpressionofKLK2andMYCgenes[1].ABBV-744(90nM;0~72h;LNCaPcells)inducescellcyclearrestinG1followedbysenescence[1].WesternBlotAnalysis[1]CellLine:LNCaPcellsConcentration:90nMIncubationTime:0~24hoursResult:DownregulatedtheexpressionofKLK2andMYCgenes.CellCycleAnalysis[1]CellLine:LNCaPcellsConcentration:90nMIncubationTime:0~72hoursResult:InducedcellcyclearrestinG1followedbysenescence.体内研究ABBV-744(4.7mg/kg;oralgavage;28days)causesadelayintumorgrowthanddisplaysequivalentorbetterantitumoractivitycomparedwithABBV-075[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEABBV-744(30mg/kg;14days)isabletoproducesignificantantitumoractivity.ABBV-744(30mg/kg)triggersareductioninplateletsofonly20%[1].AnimalModel:MiceDosage:4.7mg/kg(PharmacokineticAnalysis)Administration:Oralgavage;28daysResult:CausedadelayintumorgrowthanddisplayedequivalentorbetterantitumoractivitycomparedwithABBV-075.AnimalModel:Sprague-DawleyratsDosage:30mg/kg(PharmacokineticAnalysis)Administration:14daysResult:Producedsignificantantitumoractivity.户使⽤本产品发表的科研⽂献•Cell.2021Apr15;184(8):2167-2182.e22.•Science.2020Apr24;368(6489):387-394.•Analysis&Sensing.22June2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FaivreEJ,etal.SelectiveinhibitionoftheBD2bromodomainofBETproteinsinprostatecancer.Nature.2020;578(7794):306-310.McePdfHeightCaution:Producthasnotbe