MPT0B392-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMPT0B392Cat.No.:HY-101287CASNo.:1346169-92-3分⼦式:C₁₉H₂₀N₂O₆S分⼦量:404.44作⽤靶点:Microtubule/Tubulin;JNK;Apoptosis;Caspase作⽤通路:CellCycle/DNADamage;Cytoskeleton;MAPK/ERKPathway;Apoptosis储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(247.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4726mL12.3628mL24.7255mL5mM0.4945mL2.4726mL4.9451mL10mM0.2473mL1.2363mL2.4726mL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%salineSolubility:2.5mg/mL(6.18mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性MPT0B392⼀种⼝服活性的喹啉衍⽣物，作⽤于c-JunN末端激酶(JNK)和apoptosis的激活剂。MPT0B392抑制微管蛋⽩聚合，通过激活JNK诱导细胞有丝分裂停滞，线粒体膜电位丧失和caspases裂解，最终导致细胞凋亡。MPT0B392⼀种新型微管解聚剂，可增强西罗司对耐药急性⽩⾎病细胞和多药耐药细胞系的细胞毒性。IC50&TargetJNKCaspase体外研究MPT0B392(B392)(0.001-0.1μM;24and48hours)inhibitsthecellviabilityofHL60,MOLT-4,andCCRF-CEMcellswithIC50sof0.02μM,0.03μMand0.02μM,respectively[1].MPT0B392(0.1μM;48hours)inducesapoptosisinHL60cancercells[1].MPT0B392(0.1μMfor6-48hours;0.01-0.1μMfor24and48hours)triggerscellsarrestintheG2/Mphase,followedbyaccumulationinsubG1phaseinaconcentrationandtime-dependentmanner[1].MPT0B392(0.1μM;48hours)increasesthephosphorylationofBcl-2,Mcl-1SanddecreasesinMcl-1L[1].CellViabilityAssay[1]CellLine:HL60(acutepromyelocyticleukemia),MOLT-4(acutelymphoblasticleukemia),CCRF-CEM(acutelymphoblasticleukemia)cellsConcentration:0.001,0.003,0.01,0.03,0.1μMIncubationTime:24and48hoursResult:Inhibitedthecellviability.ApoptosisAnalysis[1]CellLine:HL60cellsConcentration:0.1μMIncubationTime:48hoursResult:Inducedapoptosisincancercells.CellCycleAnalysis[1]CellLine:HL60cellsConcentration:0.1μMor0.01,0.03,0.1μMIncubationTime:0.1μMfor6-48hours;0.01-0.1μMfor24and48hoursResult:TriggeredcellsarrestintheG2/Mphase,followedbyaccumulationinsubG1phaseinaconcentrationandtime-dependentmanner.WesternBlotAnalysis[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HL60cellsConcentration:0.1μMIncubationTime:48hoursResult:IncreasedthephosphorylationofBcl-2,Mcl-1SanddecreasedinMcl-1L.体内研究TheeffectsofMPT0B392(oralgavage;50mg/kgor100mg/kgfor12or14days)showsrelativepotentanti-leukemiaactivityinavivoxenograftmodel[1].AnimalModel:Severecombinedimmunodeficient(SCID)mice[1]Dosage:50mg/kgor100mg/kgAdministration:Oralgavage;12or14daysResult:Resultedinsignificanttumorgrowthdelay(83.3%)andtumorvolumeinhibitionwithoutlossofbodyweight.REFERENCES[1].ChaoMW,etal.Anoralquinolinederivative,MPT0B392,causesleukemiccellsmitoticarrestandovercomesdrugresistantcancercells.Oncotarget.2017Apr,8(17):27772-27785.McePdfHeightCaution:Producthasnotbeenf