Proxalutamide-GT0918-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEProxalutamideCat.No.:HY-103184CASNo.:1398046-21-3Synonyms:GT0918;Pruxelutamide分⼦式:C₂₄H₁₉F₄N₅O₂S分⼦量:517.5作⽤靶点:AndrogenReceptor;SARS-CoV作⽤通路:Others;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(193.24mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9324mL9.6618mL19.3237mL5mM0.3865mL1.9324mL3.8647mL10mM0.1932mL0.9662mL1.9324mL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(4.83mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.83mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.83mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Proxalutamide(GT0918)具有⼝服活性的雄激素受体(AR)的拮抗剂。Proxalutamide(GT0918)可⽤于前列腺癌和COVID-19的研究。IC50&TargetAndrogenReceptor[1].体外研究Proxalutamide(GT0918)down-regulatesARproteinlevelinprostatecancercells[1].ProxalutamidecanovercometheresistanceofprostaticcancercellsbydownregulatingtheexpressionofARgenes[4].Proxalutamide(GT0918,0-200μM)dose-dependentlyinhibitscellviabilityinLNCaPand22RV1[5].CellViabilityAssay[5].CellLine:FourhumanPCacelllines,LNCaP,22RV1,PC3andDU145.Concentration:1,2,5,10,20,50,100,and200μM.IncubationTime:Upto72h.Result:PreferentiallyaffectedAR-positivePCacells(IC50valuesfrom6.90to32.07μM)overAR-negativecells(IC50>200μM).体内研究Theeliminationhalf-life(t1/2)ofproxalutamideinratsisapproximately2hregardlessofwhetheritisadministeredbytheintragastricortheintravenousroute.Themaximumplasmaconcentrationofproxalutamide(Cmax)couldreach2μg/mLorhigher,andtheoralabsolutebioavailability(F)wasapproximately80%[4].AnimalModel:Rats[4].Dosage:20mg/kg(PharmacokineticAnalysis).Administration:Intragastrically.Result:T1/2=2handF%=80%REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].YouzhiTong,etal.Abstract614:Proxalutamide(GT0918),apotentandrogenreceptorpathwayinhibitor.CancerResearch.AACRAnnualMeeting2014;April5-9,2014;SanDiego,CA.[2].YangM,etal.MicroenvironmentalpH-modifiedsoliddispersionstoenhancethedissolutionandbioavailabilityofpoorlywater-solubleweaklybasicGT0918,adevelopinganti-prostatecancerdrug:preparation,characterizationandevaluationinvivo.IntJ[3].MonitoringEditor,etal.ProxalutamideSignificantlyAcceleratesViralClearanceandReducesTimetoClinicalRemissioninPatientswithMildtoModerateCOVID-19:ResultsfromaRandomized,Double-Blinded,Placebo-ControlledTrial.Cureus.2021Feb;13([4].HuaSang,etal.Quantitativedeterminationofproxalutamideinratplasmaandtissuesusingliquidchromatography/tandemmassspectrometry.RapidCommunMassSpectrom.2021Feb15;35(3):e9003.[5].FengQu,etal.Metabolomicprofilingtoevaluatetheefficacyofproxalutamide,anovelandrogenreceptorantagonist,inprostatecancercells.InvestNewDrugs.2020Oct;38(5):1292-1302.McePdfHeightCaution:Producth