Anticancer-agent-207-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEAnticanceragent207Cat.No.:HY-163515分子式: C₂₉H₃₉FN₄O₂分子量: 494.64作用靶点: Ras作用通路: GPCR/GProtein;MAPK/ERKPathway储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Anticanceragent207(compound10b)是一种有效的抗癌剂。Anticanceragent207与NRASrG4结合，KD值为2.31µM。Anticanceragent207表现出细胞毒性并降低NRAS蛋白的表达。Anticanceragent207显示出抗肿瘤活性[1]。IC50&TargetNRASrG42.31μM(Kd)体外研究Anticanceragent207(48h)showscytotoxicityforNRAS-mutantmelanomaSK-MEL-2withanIC50valueof2.0µM[1].Anticanceragent207(0,0.5,1.0µM;72h)decreasestheexpressionofNRASprotein[1].Anticanceragent207(0,0.13,0.25µM;10days)inhibitsthecolonyformationofSK-MEL-2cells[1].WesternBlotAnalysis[1]CellLine:SK-MEL-2cellsConcentration:0,0.5,1.0µMIncubationTime:72hResult:DecreasedtheexpressionofNRASproteininadose-dependentmanner.CellProliferationAssay[1]CellLine:MCF-7,HepG2,HL60,A375cells1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEConcentration:0-100µMIncubationTime:48hResult:ShowedcytotoxicitywithIC50sof4.1,1.5,2.7,4.5µMforMCF-7,HepG2,HL60,A375cells,respectively.体内研究Anticanceragent207(1mg/kg;i.p.;everydayfor21days)inhibitstumorgrowthinvolumeandweightinmice[1].AnimalModel:Six-week-oldmaleBALB/Cnudemice(SK-MEL-2xenograftmousemodel)[1]Dosage:1mg/kgAdministration:I.p.;everydayfor21daysResult:Suppressedtumorgrowthinvolumeandweightinthexenograftmousemodeltime-dependently.REFERENCESJia-WeiSun,etal.Design,synthesis,andevaluationofnovelquindolinederivativeswithfork-shapedsidechainsasRNAG-quadruplexstabilizersforrepressingoncogeneNRAStranslation.EuropeanJournalofMedicinalChemistry.2024,271(5):116406.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82