Aromatase-IN-8-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAromatase-IN-8Cat.No.:HY-180535CASNo.:1244904-19-5分⼦式:C₁₇H₁₉ClN₄S分⼦量:346.88作⽤靶点:CytochromeP450作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Aromatase-IN-8⼀种选择性的aromatase抑制剂，其对aromatase活性的半数抑制浓度(IC50)为0.05µM。Aromatase-IN-8对雌激素受体阳性乳腺癌细胞系具有选择性抗增殖作⽤，同时对⾮肿瘤细胞⽆毒性。Aromatase-IN-8可抑制雌激素活性、提⾼酮⽔平，并下调雌激素受体的表达与磷酸化。Aromatase-IN-8可⽤于三乳腺癌研究[1]。IC50&TargetAromatase0.05μM(IC50)体外研究Aromatase-IN-8(compound17)(72h)displaysprominentanticancereffectsinER+breastcancercelllines(T47DandMCF-7cells)andtriple-negativebreastcancercellline(MDA-231cells)withIC50=42.90,79.43and>100µM[1].Aromatase-IN-8(6.25-100µM,24and72h)reducescellviabilityeffectscorrelatewithincreasingdosageinMCF-7cellsandMDA-MB-231cells[1].Aromatase-IN-8(0-50μM,24h)reducesERαandERβproteinlevelsinMCF-7cells[1].Aromatase-IN-8(6.25-50μM,8h)revealslow17β-estradiolandestronesmallsuppressiveeffectsonestrogensynthesisleadstoamoreabundantaccumulationoftestosteroneatconcentrationsabove12.5µMinMCF-7cells[1].Aromatase-IN-8downregulatesfattyaciddegradation,upregulatespantothenateandCoAbiosynthesis,valineandsphingosineaccumulationandhasthestronganticancereffectsathigherdosesinMCF-7cells[1].WesternBlotAnalysis[1]CellLine:MCF-7cells1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:12.5,25and50μMIncubationTime:24hResult:Reducedtheexpressionofbothnon-phosphorylatedandphosphorylatedErαandErβinadose-dependentmanner.REFERENCES[1].MaiuthedA,etal.Anintegratedcomputational,invitroandmetabolomicsapproachtothediscoveryofnovelaromataseinhibitorswithanti-breastcanceractivities.SciRep.2025Nov17;15(1):40230.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400