Fluorizoline-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFluorizolineCat.No.:HY-114989CASNo.:1362243-70-6分⼦式:C₁₅H₈Cl₂F₃NS分⼦量:362.2作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(138.05mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7609mL13.8045mL27.6091mL5mM0.5522mL2.7609mL5.5218mL10mM0.2761mL1.3805mL2.7609mL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(6.90mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.90mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.90mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Fluorizoline选择性地直接结合到prohibitin1(PHB1)和2(PHB2)，并诱导凋亡。Fluorizoline通过上调NOXA和BIM降低慢性淋巴细胞性⽩⾎病(CLL)细胞的活⼒。Fluorizoline以p53⾮依赖性⽅式发挥抗肿瘤作⽤。体外研究Fluorizoline(1.25-20μM;24hours)inducesapoptosisinprimaryCLLcellsexvivo[1].Fluorizoline(5-10μM;48hours)causesanincreaseofNOXAproteinlevels[1].FluorizolinereducesthepercentageofviablenormalBandTcells(48.6%and82.8%ofviablecellsat24hoursoftreatmentwith10μMFluorizolineinnormalCD19+andCD3+populations,respectively)withmeanEC50valuesof10.9μMand19.1μMat24hoursfornormalBandTcells,respectively[1].ApoptosisAnalysis[1]CellLine:PrimaryCLLcellsConcentration:1.25to20μMIncubationTime:24hoursResult:Stronglyreducedcellviabilityandinducedapoptosisinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:PrimaryCLLcellsConcentration:5,10μMIncubationTime:48hoursResult:CausedanincreaseofNOXAproteinlevels.体内研究Fluorizoline(15mg/kg;ip;threetimesaweekforfiveweeks)becomesveryrapidly(3weeks)leukemic,asreflectedbytheincreaseinthepercentageandthenumberofCD5+CD19+CLLcellsinthebloodin6-week-oldrecipientC57BL/6Eμ-TCL1mousemodelofCLL.Fluorizolinedoesnotinduceapoptosisinvivo.Fluorizolinedoesnotcontroldiseasedevelopmentinthespleenasindicatedbyenlargedspleens[2].REFERENCES[1].AnaMCosialls,etal.Theprohibitin-bindingcompoundfluorizolineinducesapoptosisinchroniclymphocyticleukemiacellsthroughtheupregulationofNOXAandsynergizeswithibrutinib,5-aminoimidazole-4-carboxamideribosideorvenetoclax.Haematologica.20172/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESep;102(9):1587-1593.[2].MarinaWierz,etal.Theprohibitin-bindingcompoundfluorizolineinducesapoptosisinchroniclymphocyticleukemiacellsexvivobutfailstopreventleukemiadevelopmentinamurinemodel.Haematologica.2018Apr;103(4):e154-e157.McePdfHeightCaution:Producthasnotbeenfullyval