DRB18-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDRB18Cat.No.:HY-145963分⼦式:C₂₂H₂₃ClN₂O₂分⼦量:382.88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:50mg/mL(130.59mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6118mL13.0589mL26.1178mL5mM0.5224mL2.6118mL5.2236mL10mM0.2612mL1.3059mL2.6118mL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。BIOLOGICALACTIVITY⽣物活性DRB18⼀种有效的葡萄糖转运蛋⽩(GLUT)泛抑制剂。DRB18通过改变葡萄糖相关途径中代谢产物的丰度来改变A549细胞中的能量相关代谢。DRB18最终可导致细胞阻滞在G1/S期，增加氧化应激和坏死细胞死亡。DRB18具有抗肿瘤活性[1]。IC50&TargetGLUT[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究DRB18(0-10μM;30min)reducesglucoseuptakeinGLUT1-4-expressedHEK293celllinesinadose-dependentmannerwithIC50svaryingfrom~900nMto~9μM[1].DRB18(5and10μM;72hours)causescellcyclearrestintheG1/Sphasetransition[1].DRB18(5and10μM;72hours)increasesROSlevelsinA549cells[1].DRB18(5and10μM;72hours)reducesexpressionofglycosylatedGLUT1andGLUT2-4inA549cellsinadose-dependentmanner[1].CellProliferationAssayCellLine:GLUT1-4-expressedHEK293celllines[1]Concentration:0-10μMIncubationTime:30minResult:Reducedglucoseuptakeinthesecelllinesinadose-dependentmannerwithIC50svaryingfrom~900nMto~9μM.CellCycleAnalysisCellLine:A549[1]Concentration:5and10μMIncubationTime:72hoursResult:CausedcellcyclearrestintheG1/Sphasetransition.WesternBlotAnalysisCellLine:A549[1]Concentration:5and10μMIncubationTime:72hoursResult:ReducedexpressionofglycosylatedGLUT1andGLUT2-4inA549cellsinadose-dependentmanner.WesternBlotAnalysisCellLine:A549[1]Concentration:5and10μMIncubationTime:72hoursResult:ReducedexpressionofglycosylatedGLUT1andGLUT2-4inA549cellsinadose-dependentmanner.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究DRB18(10mg/kg;IP;thriceaweekfor5weeks)inhibitstumorsvolumeby44%andtumorsweightby43%[1].AnimalModel:MaleNU/Jnudemice(3-4weeks;tumorcell-injected)[1]Dosage:10mg/kgAdministration:IP;thriceaweekfor5weeksResult:Thetumorswere44%smallerbyvolumeand43%smallerbyweight,alsoshowedDRB18decreasedexpressionofGLUT1-4(Fig.5f)andreducedproliferativecapacitywithinthexenograftedtumor.REFERENCES[1].ShriwasP,RobertsD,LiY,etal.Asmall-moleculepan-classIglucosetransporterinhibitorreducescancercellproliferationinvitroandtumorgrowthinvivobytargetingglucose-basedmetabolism.CancerMetab.2021;9(1):14.Published2021Mar26.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica