Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMPT0B392Cat.No.:HY-101287CASNo.:1346169-92-3分?式:C??H??N?O?S分?量:404.44作?靶點:Microtubule/Tubulin;JNK;Apoptosis;Caspase作?通路:CellCycle/DNADamage;Cytoskeleton;MAPK/ERKPathway;Apoptosis儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(247.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4726mL12.3628mL24.7255mL5mM0.4945mL2.4726mL4.9451mL10mM0.2473mL1.2363mL2.4726mL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。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.5mg/mL(6.18mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性MPT0B392?種?服活性的喹啉衍?物，作?于c-JunN末端激酶(JNK)和apoptosis的激活劑。MPT0B392抑制微管蛋?聚合，通過激活JNK誘導細胞有絲分裂停滯，線粒體膜電位喪失和caspases裂解，最終導致細胞凋亡。MPT0B392?種新型微管解聚劑，可增強西羅司對耐藥急性??病細胞和多藥耐藥細胞系的細胞毒性。IC50&TargetJNKCaspase體外研究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?邊的抑制劑?師www.MedChemECellLine:HL60cellsConcentration:0.1μMIncubationTime:48hoursResult:IncreasedthephosphorylationofBcl-2,Mcl-1SanddecreasedinMcl-1L.體內(nèi)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