APTO-253-LOR-253-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAPTO-253Cat.No.:HY-16291CASNo.:916151-99-0Synonyms:LOR-253;LT-253分⼦式:C₂₂H₁₄FN₅分⼦量:367.38作⽤靶点:c-Myc;KLF;Apoptosis作⽤通路:Apoptosis;MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:60mg/mL(163.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7220mL13.6099mL27.2198mL5mM0.5444mL2.7220mL5.4440mL10mM0.2722mL1.3610mL2.7220mL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:2.3mg/mL(6.26mM);Suspendedsolution;Needultrasonicandwarming2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.66mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性APTO-253(LOR-253)⼀种⼩分⼦，可抑制c-Myc表达，稳定G-四链体DNA并诱导急性髓样⽩⾎病细胞的细胞周期停滞和凋亡。APTO-253通过诱导Kruppel-likefactor4(KLF4)抑癌因⼦介导抗癌活性。APTO-253具有抗关节炎活性。IC50&Targetc-Myc[1];KLF4[2]体外研究APTO-253(LOR-253)isaninducerofKLF4.APTO-253(5μM)inducesKLF4expression,andenhancesapoptosisinducedbyNSC119875inbothSKOV3andOVCAR3cells.APTO-253(5μM)alsoleadstoG1phasearrestandreducesSandG2/MphasecellsinSKOV3andOVCAR3cells[1].APTO-253iscytotoxictoRajiandRaji/253Rcelllines,withIC50sof105±2.4nMand1387±94nM,respectively.APTO-253(0.5μM)alsocausesDNAdamageinRajicells.BRCA1/2deficientcellsarehypersensitivetoAPTO-253.ABCG2overexpressedHEK-293cellsareresistanttoAPTO-253andinhibitionofABCG2reversesresistancetoAPTO-253inRaji/253R[2].APTO-253suppressestheproliferationofacutemyeloidleukemia(AML)celllinesandvariousformsoflymphomacelllineswithIC50srangingfrom57nMto1.75µM.APTO-253(500nM)alsocausesG0/G1cellcyclearrest,inducesapoptosis,anddownregulatesMYCRNAandproteinexpressioninAMLlines.APTO-253(500nM)leadstoDNAdamageresponsepathwaysinMV4-11cells.Futhermore,APTO-253isapotentstabilizerofGquadruplex(G4)motifs,anddemonstratesthegreatestpropensityforstabilizingtheMYCG4sequences[3].体内研究APTO-253(LOR-253;15mg/kg;IV;twiceperdayfor2consecutivedaysperweekfor14days)hasantiarthriticactivityinaCIAmodel[3].AnimalModel:DBA/1Jmalemice(6weeks)withcollageninducedarthritis(CIA)[3]Dosage:15mg/kgAdministration:IV;twiceperdayfor2consecutivedaysperweekfor14daysResult:Demonstratedsignificantpreventiveandtherapeuticactivityonarthritisformation.户使⽤本产品发表的科研⽂献•AnnRheumDis.2020Nov2;annrheumdis-2020-218189.•NatCommun.2019Sep25;10(1):4369.•JCIInsight.2022Jul19;e160688.•Genes(Basel).2021,12(4),539.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•JDiabetesRes.15Sep2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LocalA,etal.APTO-253StabilizesG-quadruplexDNA,InhibitsMYCExpression,andInducesDNADamageinAcuteMyeloidLeukemiaCells.MolCancerTher.2018Jun;17(6):1177-1186.[2].HongyingZhang,etal.Inhibitionofc-MycByApto-253AsanInnovativeTherapeuticApproachtoInduceCellCycleArrestandApoptosisinAcuteMyeloidLeukemia.Blood2016128:1716.[3].HarukaTsuchiya,etal.Parsingmultiomicslandscapeofactivatedsynovialfibroblastshighlightsdrugtargetslinkedtogeneticriskofrheumatoidarthritis.AnnRheumDis.2020Nov2;annrheumdis-2020-218189.McePdfHeightCautio