Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHUHS015Cat.No.:HY-100199CASNo.:1453097-13-6分?式:C??H??N?O分?量:318.37作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥34mg/mL(106.79mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1410mL15.7050mL31.4100mL5mM0.6282mL3.1410mL6.2820mL10mM0.3141mL1.5705mL3.1410mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(7.85mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.85mM);Clearsolution3.請依序添加每種溶劑：50%PEG300>>50%salineSolubility:5mg/mL(15.70mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性HUHS015?種?效的PCA-1/ALKBH3抑制劑，對PCA-1作?的IC50值為0.67μM[1]。IC50&TargetIC50:0.67μM(PCA-1)[1]體外研究HUHS015significantlysuppressesthegrowthofDU145cells,whicharehumanhormone-independentprostatecancercells[1].體內(nèi)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: