BP-1-102-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBP-1-102Cat.No.:HY-100493CASNo.:1334493-07-0分⼦式:C₂₉H₂₇F₅N₂O₆S分⼦量:626.59作⽤靶点:STAT作⽤通路:JAK/STATSignaling;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥33mg/mL(52.67mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5959mL7.9797mL15.9594mL5mM0.3192mL1.5959mL3.1919mL10mM0.1596mL0.7980mL1.5959mL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:≥2.5mg/mL(3.99mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.99mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BP-1-102有⼝服活性的转录因⼦Stat3的⼩分⼦抑制剂，其IC50值为6.8μM。IC50&TargetSTAT36.8μM(IC50)体外研究BP-1-102bindsStat3withanaffinityKDof504nM.BP-1-102inhibitsStat3DNA-bindingactivityinvitro,withanIC50valueof6.8±0.8μM.ItblocksStat3-phospho-tyrosinepeptideinteractionsandStat3activationat4-6.8μM,andselectivelyinhibitsgrowth,survival,migration,andinvasionofStat3-dependenttumorcells.BP-1-102-mediatedinhibitionofaberrantlyactiveStat3intumorcellssuppressestheexpressionofc-Myc,CyclinD1,Bcl-xL,Survivin,VEGF,andKrüppel-likefactor8[1].体内研究MicetherapeuticallygivenBP-1-102,anorallybioavailablecompoundtargetingSTAT3/NF-kBactivationandcross-talk,exhibitreducedcolontumorigenesisanddiminishedexpressionofSTAT3/NF-kB-activatingcytokinesintheneoplasticareas[2].BP-1-102isorallybioavailableandthattheagentaccumulatesintumortissuesatlevelssufficienttoinhibitaberrantlyactiveStat3functionsandinhibittumorgrowth[1].PROTOCOLCellAssay[1]Proliferatingcellsin6-or96-wellplatesaretreatedoncewith0-30μMBP-1-102for24horwith10μMBP-1-102forupto96h.Viablecellsarecountedbytrypanblueexclusion/phase-contrastmicroscopyorassessedbyacellproliferationkit[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:AthymicnudemicewithestablishedtumorsaregroupedandthengivenBP-1-102(in0.05%DMSOinAdministration[1]water)at1or3mg/kg(i.v.)every2orevery3dor3mg/kg(oralgavage,100μL)everydayfor15or20d.Animalsaremonitoredeveryday,andtumorsizesaremeasuredwithcalipersandbodyweightsaretakenevery2or3d.Foreachtreatmentgroup,thetumorvolumesforeachsetofmeasurementsarestatisticallyanalyzedincomparisonwiththecontrolgroupusingapairedTtest[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2022Nov29;13(1):7345.•Oncogene.2018Nov;37(45):5952-5966.•CellCommunSignal.2020Jul8;18(1):104.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangX,etal.Orallybioavailablesmall-moleculeinhibitoroftranscriptionfactorStat3regresseshumanbreastandlungcancerxenografts.ProcNatlAcadSciUSA.2012Jun12;109(24):9623-8.[2].DeSimoneV,etal.Th17-typecytokines,IL-6andTNF-αsynergisticallyactivateSTAT3andNF-kBtopromotecolorectalcancercellgrowth.Oncogene.2015Jul;34(27):3493-503.McePdfHeightCaution:Pr