PFK-158-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPFK-158Cat.No.:HY-12203CASNo.:1462249-75-7分⼦式:C₁₈H₁₁F₃N₂O分⼦量:328.29作⽤靶点:Autophagy;Apoptosis作⽤通路:Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(91.38mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0461mL15.2304mL30.4609mL5mM0.6092mL3.0461mL6.0922mL10mM0.3046mL1.5230mL3.0461mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2mg/mL(6.09mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2mg/mL(6.09mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2mg/mL(6.09mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PFK-158⼀种有效的，选择性的PFKFB3抑制剂，IC50值为137nM。PFK-158可减少癌细胞中葡萄糖的摄取，ATP的产⽣，乳酸的释放，并诱导细胞凋亡和⾃噬。PFK-158具有⼴泛的抗肿瘤活性。PFK-158还可以增强Colistin对细的抵抗⼒。IC50&TargetIC50:137nM(PFKFB3)[1][3]体外研究PFK-158(10µM;24hours;OV2008andC13cells)combinedwithCarboplatin(CBPt;77-453μM)resultsinsignificantincreaseinapoptosisinC13(45%)andOV2008cells(24.6%)[1].PFK-158(0-10µM;24hours;C13andHeyA8MDRcells)treatmentresultsinadose-dependentdecreasein

p-PFKFB3,p-cPLA2andlipiddroplet(LD)levels[1].PFK-158(10μM;24hours)hassynergisticanti-proliferativeeffectsinvitrowhencombinedwithCisplatinin

C13andHeyA8MDRcellscomparedtoOV2008andHeyA8,respectively[1].PFK-158(0‐10μM;24h)treatmentshowsadose-dependentdownregulationofp62/SQSTM1andupregulationofLC3BII,twomarkersofautophagyinduction,inbothC13andHeyA8MDRcells.PFK-158treatmentalsoreducesthenumbersofLDs[1].ApoptosisAnalysis[1]CellLine:OV2008andC13cellsConcentration:10µMIncubationTime:24hoursResult:CombinedwithCarboplatin(CBPt)treatmentresultedinsignificantincreaseinapoptosis.WesternBlotAnalysis[1]CellLine:C13andHeyA8MDRcellsConcentration:0µM,5µM,10µMIncubationTime:24hoursResult:Demonstratedadose-dependentdecreaseinp-PFKFB3,p-cPLA2andlipiddroplet(LD)levels.体内研究PFK-158(15mg/kg;intraperitonealinjection;onceaweek;for4weeks;femaleathymicnudemice)plus2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECBPt(51mg/kg)treatmentleadstosignificantlyenhancedantitumoractivityinagynecologiccancermousemodel[1].AnimalModel:Femaleathymicnudemice(nu/nu)(5-6weeksold)injectedwithHeyA8MDRcells[1]Dosage:15mg/kgAdministration:Intraperitonealinjection;onceaweek;for4weeksResult:Amarkedreductionoftumorgrowthwasobservedinthecombinationtreatment.户使⽤本产品发表的科研⽂献•Cells.2021,10(7),1679.•JBiolChem.2019Jul5;294(27):10530-10543.•InfectDrugResist.2021Jun9;14:2143-2154.•ResearchSquarePreprint.2021Nov.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MondalS,etal.TherapeutictargetingofPFKFB3withanovelglycolyticinhibitorPFK158promoteslipophagyandchemosensitivityingynecologiccancers.IntJCancer.2019Jan1;144(1):178-189.[2].ZhangY,etal.SynergisticEffectofColistinCombinedwithPFK-158againstColistin-ResistantEnterobacteriaceae.AntimicrobAgentsChemother.2019Jun24;63(7).pii:e00271-19.[3].PooranChand,etal.Pfkfb3inhibitorandmethodsofuseasananti-cancertherapeutic.WO2013148228A1.McePdfHeightCauti