NAZ2329-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENAZ2329Cat.No.:HY-103693分⼦式:C₂₁H₁₈F₃NO₄S₃分⼦量:501.56作⽤靶点:Phosphatase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(199.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9938mL9.9689mL19.9378mL5mM0.3988mL1.9938mL3.9876mL10mM0.1994mL0.9969mL1.9938mL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(4.98mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.98mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.98mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NAZ2329受体型蛋⽩质酪氨酸磷酸酶(RPTPs)R5亚家族的第⼀个细胞可渗透抑制剂，相对于其他PTPs，它变构且优先抑制PTPRZ(hPTPRZ1的IC50=7.5µM)和PTPRG(hPTPRGIC50=4.8µM)。NAZ2329与PTPRZ的D1结构域结合，相对于PTPRZ整个(D1+D2)⽚段，其更有效地抑制PTPRZ1-D1⽚段，其IC50为1.1µM。NAZ2329可有效抑制胶质母细胞瘤细胞的肿瘤⽣长并抑制⼲细胞样特性。IC50&TargetIC50:7.5µM(PTPRZ),4.8µM(PTPRG),35.7µM(PTPRA),56.7µM(PTPRM),23.7µM(PTPRS),35.4µM(PTPRB),15.2µM(PTPN6),14.5µM(PTPN1)[1]体外研究NAZ2329(0-25µM;48hours)dose-dependentlyinhibitscellproliferationandmigrationinallcelllines(ratglioblastomacellsbearingC6cloneandhumanU251glioblastomacells)[1].NAZ2329(25µM;0-90min)obviouslypromotesthephosphorylationlevelofpaxillinatTyr-118site,leadingtoinhibitionforPTPRsubstrate[1].CellProliferationAssay[1]CellLine:RatglioblastomacellsbearingC6clone,humanU251glioblastomacellsConcentration:0µM,6.3µM,12.5µM,25µMIncubationTime:48hoursResult:Exertedinhibitionincellproliferationandmigrationinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:RatglioblastomacellsbearingC6cloneConcentration:25µMIncubationTime:0min,15min,30min,60min,90minResult:PromotedthephosphorylationlevelofpaxillinatTyr-118site.体内研究NAZ2329(22.5mg/kg;intraperitonealinjection;twiceperweek;40days)alonehasamoderateinhibitoryeffect.However,thecombinationofTemozolomideandNAZ2329exertsasignificantlyincreasedinhibitionoftumorgrowthcomparedwiththecontrolgroup,theNAZ2329monotherapygroupandtheTemozolomidemonotherapygroup[1].AnimalModel:FemaleBALB/c-nu/numiceaged4week-oldbearingparentalorPtprz-knockdownC6cells[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:22.5ꢀmg/kg;Temozolomide(TMZ,50ꢀmg/kg)Administration:Intraperitonealinjection;twiceperweek;40daysResult:ThecombinationofNAZ2329andTMZsignificantlydelayedtumorgrowthcomparedtoNAZ2329orTMZalone.REFERENCES[1].AkihiroFujikawa,etal.TargetingPTPRZinhibitsstemcell-likepropertiesandtumorigenicityinglioblastomacells.SciRep.2017Jul17;7(1):5609.McePdfHeightCaution:Producthasnotbeenfull