AHR-antagonist-5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAHRantagonist5Cat.No.:HY-136220CASNo.:2247953-39-3分⼦式:C₂₅H₂₇Cl₃FN₇分⼦量:550.89作⽤靶点:ArylHydrocarbonReceptor作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(181.52mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8152mL9.0762mL18.1524mL5mM0.3630mL1.8152mL3.6305mL10mM0.1815mL0.9076mL1.8152mL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(4.54mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性AHRantagonist5有效的，具有⼝服活性的芳⾹烃受体(AHR)拮抗剂，IC50为<0.5μM。AHRantagonist5联合检测点抑制剂anti-PD-1对肿瘤⽣长有抑制作⽤，详细信息请参见专利WO2018195397，example39。体内研究TumorgrowthinhibitionisstatisticallysignificantwithAHRantagonist5assingle.AHRantagonist5(10mg/kg;p.o.;everydayfor3weeks)combinationwithanti-PD-1significantlyinhibitedtumorgrowthinhibitioncomparedtotheanti-PD-1alone[1].AnimalModel:Balb/cMice(MouseColorectalCancerModelCT26)[1]Dosage:10mg/kg(combinationwithanti-PD-1)Administration:P.o.;everydayfor3weeksResult:Significantlyinhibitedtumorgrowthinhibition.REFERENCES[1].AlfredoC.Castro,etal.Indoleahrinhibitorsandusesthereof.WO2018195397A2.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;