Letrozole-CGS-20267-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELetrozoleCat.No.:HY-14248CASNo.:112809-51-5Synonyms:CGS20267分⼦式:C₁₇H₁₁N₅分⼦量:285.3作⽤靶点:Aromatase;Autophagy作⽤通路:Others;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(175.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5051mL17.5254mL35.0508mL5mM0.7010mL3.5051mL7.0102mL10mM0.3505mL1.7525mL3.5051mL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:≥2.08mg/mL(7.29mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.29mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.29mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Letrozole(CGS20267)⼀种有效的，选择性的，可逆的和具有⼝服活性的⾮甾体类芳⾹化酶(aromatase)抑制剂，IC50值为11.5nM。Letrozole选择性抑制雌激素的⽣物合成，可⽤于乳腺癌的研究。IC50&TargetIC50:11.5nM(aromatase)[1]体外研究Letrozole(0.1-100nM;24-96h)significantlyinhibitsgrowthoftheMCF-7epithelialbreastcancercellsinadose-andtime-dependentmanner[2].Letrozole(10nM)significantlysuppressesthestimulatoryeffectsof4-androstene-3,17-dioneortestosterone

onMCF-7cellproliferation[2].Letrozole(10nM;24-48h)suppressesthelevelsofsecretedmetalloproteinases(MMP‐2andMMP‐9)inMCF-7cells[2].CellViabilityAssay[2]CellLine:MCF-7cellsConcentration:0.1,1,10,100nMIncubationTime:24,48,96hoursResult:Inhibitedcellsgrowthinadose-andtime-dependentmanner.体内研究Letrozole(3-300μg/kg;oralgavageoncedailyfor6weeks)exhibitsanti-tumoreffectsinrats[3].AnimalModel:Adultfemaleratsbearingmammarytumors[3]Dosage:3,10,30,100,300μg/kgAdministration:Oralgavageoncedailyfor6weeksResult:Inducedcompleteregressionofmammarytumors,withanED50of10-30μg/kg/day.户使⽤本产品发表的科研⽂献•NucleicAcidsRes.2020Nov4;48(19):10768-10784.•CancerLett.2019Dec28;467:72-84.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•EcotoxicolEnvironSaf.2021Apr27;217:112255.•MolCancerRes.2018Mar;16(3):361-377.•PLoSGenet.2022Jun29;18(6):e1010288.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BhatnagarAS,et,al.HighlyselectiveinhibitionofestrogenbiosynthesisbyCGS20267,anewnon-steroidalaromataseinhibitor.JSteroidBiochemMolBiol.1990Dec20;37(6):1021-7.[2].MitropoulouTN,et,al.Letrozoleasapotentinhibitorofcellproliferationandexpressionofmetalloproteinases(MMP-2andMMP-9)byhumanepithelialbreastcancercells.IntJCancer.2003Mar20;104(2):155-60.[3].SchieweckK,et,al.Anti-tumorandendocrineeffectsofnon-steroidalaromataseinhibitorsonestrogen-dependentratmammarytumors.JSteroidBiochemMolBiol.1993Mar;44(4-6):633-6.McePdfHeightCaution:Producthasnotbeenfully