HUHS015-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHUHS015Cat.No.:HY-100199CASNo.:1453097-13-6分⼦式:C₁₉H₁₈N₄O分⼦量:318.37作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥34mg/mL(106.79mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1410mL15.7050mL31.4100mL5mM0.6282mL3.1410mL6.2820mL10mM0.3141mL1.5705mL3.1410mL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%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(7.85mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.85mM);Clearsolution3.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:5mg/mL(15.70mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性HUHS015⼀种⾼效的PCA-1/ALKBH3抑制剂，对PCA-1作⽤的IC50值为0.67μM[1]。IC50&TargetIC50:0.67μM(PCA-1)[1]体外研究HUHS015significantlysuppressesthegrowthofDU145cells,whicharehumanhormone-independentprostatecancercells[1].体内研究HUHS015potentlysuppressesthegrowthofDU145cellsinamousexenograftmodel[1].HUHS015displays7.2%bioavailability(BA)inratsafteroraladministration[1].AnimalModel:Nudemice[1]Dosage:32mg/kgAdministration:Subcutaneousinjection;daily;6daysResult:HasinhibitoryeffectonthegrowthofsubcutaneouslyimplantedDU145,withoutlimitingweightgainsaftera6dayscontinuousadministration.REFERENCES[1].NakaoSetal.Designandsynthesisofprostatecancerantigen-1(PCA-1/ALKBH3)inhibitorsasanti-prostatecancerdrugs.BioorgMedChemLett,2014Feb15,24(4):1071-4.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: