AES-135-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAES-135Cat.No.:HY-114483CASNo.:2361659-61-0分⼦式:C₃₃H₂₉F₆N₃O₅S分⼦量:693.66作⽤靶点:HDAC作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(144.16mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4416mL7.2081mL14.4163mL5mM0.2883mL1.4416mL2.8833mL10mM0.1442mL0.7208mL1.4416mL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>>90%cornoilSolubility:≥2.5mg/mL(3.60mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性AES-135⼀种于羟肟酸的泛HDAC抑制剂，可延长胰腺癌原位⼩⿏模型的存活时间。AES-135抑制HDAC3、HDAC6、HDAC8和HDAC11，IC50范为190-1100nM。IC50&TargetHDAC6HDAC11HDAC3HDAC8190nM(IC50)636nM(IC50)654nM(IC50)1100nM(IC50)体外研究AES-135inhibitscancercellsgrowthwithIC50valuesof2.3µM,1.4µM,0.27µM,0.94µM,1.9µM,2.72µM,2.1µM,15.0µM,1.6µMand19.2µMforBT143,BT189,D425,D458,MV4-11,MOLM-13,MDA-MB-231,K562,PC-3andMRC-9cells,respectively[1].体内研究AES-135(50mg/kg;intraperitonealinjection;5daysaweek;for1month)treatmentsignificantlyincreasessurvivalofC57Bl/6miceimplantedwithKPC2cells[1].NSGmicearedosedwithasingle20mg/kgintraperitoneal(IP)injection,andbloodistakenat0.5h,1h,2h,4h,8h,and24h.AES-135achievedμMconcentrationsintheblood,reachingCmax7452ng/mL(10.74μM)within30min,whichissustainedfor8h.ThebloodconcentrationofAES-135isdosedependent,achievinganaverageof323ng/mL(0.47μM)with10mg/kgdosingand1829ng/mL(2.64μM)with40mg/kg.AES-135showsanimpressivepharmacokineticprofileinmicewithaninvivohalf-lifeof5.0h[1].AnimalModel:C57Bl/6miceinjectedwithKPC2cells[1]Dosage:50mg/kgAdministration:Intraperitonealinjection;5daysaweek;for1monthResult:Significantlyincreasedsurvivalofmice.户使⽤本产品发表的科研⽂献•CellDeathDis.2021May18;12(6):501.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ShouksmithAE,etal.IdentificationandCharacterizationofAES-135,aHydroxamicAcid-BasedHDACInhibitorThatProlongsSurvivalinanOrthotopicMouseModelofPancreaticCancer.JMedChem.2019Mar14;62(5):2651-2665.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat