BAY-876-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAY-876Cat.No.:HY-100017CASNo.:1799753-84-6分⼦式:C₂₄H₁₆F₄N₆O₂分⼦量:496.42作⽤靶点:GLUT作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(201.44mM)Methanol:1mg/mL(2.01mM;ultrasonicandwarmingandheatto60°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0144mL10.0721mL20.1442mL5mM0.4029mL2.0144mL4.0288mL10mM0.2014mL1.0072mL2.0144mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.04mM);Clearsolution2.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:5mg/mL(10.07mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性BAY-876⼀种具有⼝服活性的，选择性的葡萄糖转运蛋⽩1(GLUT1)抑制剂，IC50为2nM。BAY-876对GLUT1的选择性GLUT2，GLUT3和GLUT4的130倍以上。BAY-876还⼀种糖酵解代谢和巢癌⽣长的有效阻滞剂。IC50&TargetGLUT1GLUT2GLUT3GLUT42nM(IC50)10.08μM(IC50)1.67μM(IC50)0.29μM(IC50)体外研究BAY-876(25-75nM;24and72hours)hasthegrowth-inhibitoryeffectandleadstoadose-dependentdecreaseinnumbersofSKOV-3andOVCAR-3cells[2].CellProliferationAssay[2]CellLine:SKOV-3andOVCAR-3cellsConcentration:25,50,75nMIncubationTime:24and72hoursResult:Ledtoadose-dependentdecreaseinnumbersofSKOV-3andOVCAR-3cells.体内研究BAY-876(oraladministration;1.5-4.5mg/kg/dayfor28days)causesacleardose-dependentinhibitionoftumorigenicityinmice[2].AnimalModel:FemaleNOD-scidIL2rgnull(NSG)micecarryingSKOV-3subcutaneous(s.c.)xenografts[2]Dosage:1.5,3,4.5mg/kgAdministration:Oraladministration;daily;for28daysResult:Causedacleardose-dependentinhibitionoftumorigenicity.户使⽤本产品发表的科研⽂献•Small.2021Aug4;e2102695.•JHazardMater.16October2021,127512.•RedoxBiol.2021Jul26;46:102082.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•ExpertOpinTherPat.2022Jan9.•Cancers(Basel).2022,14(2),345.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SiebeneicherHetal.IdentificationandOptimizationoftheFirstHighlySelectiveGLUT1InhibitorBAY-876.ChemMedChem.2016Aug23.[2].MaY,etal.OvarianCancerReliesonGlucoseTransporter1toFuelGlycolysisandGrowth:Anti-TumorActivityofBAY-876.Cancers(Basel).2018Dec31;11(1).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap