Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMBM-55Cat.No.:HY-101029CASNo.:2083622-09-5分?式:C??H??FN?O?分?量:498.55作?靶點:Apoptosis作?通路:Apoptosis儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(250.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0058mL10.0291mL20.0582mL5mM0.4012mL2.0058mL4.0116mL10mM0.2006mL1.0029mL2.0058mL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(fù)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(protectfromlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性MBM-55有效的NIMA-relatedkinase2(Nek2)抑制劑，IC50值為1nM，其他激酶選擇性的20倍甚?更?，除了RSK1(IC50=5.4nM)和DYRK1a(IC50=6.5nM)。MBM-55通過誘導(dǎo)細(xì)胞周期停滯和凋亡(apoptosis)抑制癌細(xì)胞的增殖。具有抗腫瘤活性，且對??沒有明顯的毒性[1]。IC50&TargetIC50:1nM(Nek2),5.4nM(RSK1),6.5nM(DYRK1a),57nM(CHK1),91nM(GSK-3β),20nM(ABL),370nM(CDK2),441nM(CDK4),608nM(AKT1),5300nM(AuroraA)[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究MBM-55(compound42g)inhibitsMGC-803,HCT-116,Bel-7402cellsproliferationwithIC50sof0.53,0.84,7.13μM,respectively[1].MBM-55(0.5-1μM;24hours)inducesG2/Mphasearrestandaccumulationofcellswith>4NcontentinHCT-116cells[1].MBM-55(0.5-1μM;24hours)causescellapoptosisinaconcentration-dependentmannerinHCT-116cells[1].CellCycleAnalysis[1]CellLine:HCT-116cellsConcentration:0.5,1μMIncubationTime:24hoursResult:InducedG2/Mphasearrestandaccumulationofcellswith>4Ncontent.ApoptosisAnalysis[1]CellLine:HCT-116cellsConcentration:0.5,1μMIncubationTime:24hoursResult:Causedcellapoptosisinaconcentration-dependentmanner.體內(nèi)研究MBM-55(20mg/kg;i.p.;twiceadayfor21days)exhibitsgoodantitumoractivityandawell-tolerateddosescheduleinnudemicebearingHCT-116xenografts[1].MBM-55(1.0mg/kg;i.v.)treatmentshowstheCL,Vss,T1/2,AUC0-t,andAUC0-∞valuesof33.3mL/min/kg,2.53L/kg,1.72hours,495ng/h/mLand507ng/h/mL,respectively.AnimalModel:FemaleBALB/cnu/numice(5-6weeks,bearingHCT-116xenografts)[1]Dosage:20mg/kgAdministration:Intraperitonealinjection;twiceadayfor21daysResult:Significantlysuppressedtumorgrowth.AnimalModel:MaleSpragueDawley(SD)rats[1]Dosage:1.0mg/kgAdministration:IVinjection(PharmacokineticAnalysis)Result:TheCL,Vss,T1/2,AUC0-t,andAUC0-∞valueswere33.3mL/min/kg,2.53L/kg,1.72hours,495ng/h/mLand507ng/h/mL,respectively.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].XiJB,etal.Structure-baseddesignandsynthesisofimidazo[1,2-a]pyridinederivativesasnovelandpotentNek2inhibitorswithinvitroandinvivoantitumoractivities.EurJMedChem.2017Jan27;126:1083-1106.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic