Tubulin-IN-57-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemETubulin-IN-57Cat.No.:HY-178325分子式: C₂₆H₂₄N₄O₃分子量: 440.49作用靶点: Microtubule/Tubulin;Apoptosis作用通路: CellCycle/DNADamage;Cytoskeleton;Apoptosis储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Tubulin-IN-57是一种Tubulin抑制剂。Tubulin-IN-57是一种强效抗增殖剂，可抑制卵巢癌细胞的克隆形成、迁移和侵袭。Tubulin-IN-57抑制微管蛋白聚合，进而诱导SKOV3细胞发生G2/M期阻滞和凋亡(apoptosis)。在SKOV3异种移植瘤模型中，Tubulin-IN-57表现出显著的抗肿瘤活性，且未观察到明显的毒性。Tubulin-IN-57可用于卵巢癌的研究[1]。体外研究Tubulin-IN-57(CompoundY60s)(72h)exhibitspotentantiproliferativeactivity(SKOV3IC50=0.025μM;A549IC50=0.026μM)[1].Tubulin-IN-57(25-200nM,6days)inhibitsthecolonyformationandproliferationofSKOV3andA549cells[1].Tubulin-IN-57(25-200nM,0-24h)inhibitsthemigrationofSKOV3andA549cells[1].Tubulin-IN-57(25-200nM,48h)inducescellapoptosisandalterstheexpressionofapoptosis-relatedproteinsofSKOV3andA549[1].Tubulin-IN-57(25,50,100,200nM,24h)inducestheG2/MphasecellcyclearrestinSKOV3andA549cells[1].Tubulin-IN-57(10-40μM)inhibitspolymerizationanddemonstratesdose-dependentinhibitionoftubulinpolymerization,withcompleteinhibitionobservedat20μM[1].Tubulin-IN-57(20nM)causesseveremicrotubuledisruptionanddisorganizationinSKOV3[1].CellProliferationAssay[1]CellLine:SKOV3,A549cellsConcentration:25nM,50nM,100nM,200nM1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:6daysResult:Dose-dependentlyinhibitedcolonyformationinSKOV3cells.RevealedsignificantinhibitioninSKOV3cellsstartingat25nM.CellMigrationAssay[1]CellLine:SKOV3,A549cellsConcentration:25nM,50nM,100nM,200nMIncubationTime:0h,6h,12h,24hResult:Dose-dependentlyinhibitedSKOV3cellmigration.Asimilardose-dependentinhibitionwasobservedinA549cells.Resultedinadose-dependentreductioninwoundclosureinbothSKOV3andA549cellsover24h.WesternBlotAnalysis[1]CellLine:SKOV3,A549cellsConcentration:100nMIncubationTime:48hResult:Dose-dependentlydownregulatedBcl-2andupregulatedcleavedPARP,cleavedcaspase-3,andcleavedcaspase-9inbothSKOV3andA549cells.CellCycleAnalysis[1]CellLine:SKOV3,A549cellsConcentration:25nM,50nM,100nM,200nMIncubationTime:24hResult:ResultedinG2/MphasearrestinbothSKOV3andA549cells.WesternBlotAnalysis[1]CellLine:SKOV3,A549cellsConcentration:25nM,50nM,100nM,200nMIncubationTime:24hResult:Dose-dependentlyincreasedcyclinB1expressionanddecreasedCdc25cexpressioninbothcelllines.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECdc2expressionshowedcellline-specificdifferences:inSKOV3cells,thereductionwasnotapparentacrossthetreatmentrange,whereasinA549cells,Cdc2levelsremainedlargelyunchangedat50nMbutbegantodecreaseat100nM.体内研究Tubulin-IN-57(2mg/kg,4mg/kg,intravenousadministration,every2daysforatotalof12doses)inhibitstumorgrowthbysuppressingbothcellproliferationandshowsnosignificantpathologicalchangesinmice,indicatingminimaltoxicityatthetesteddosesandschedules[1].AnimalModel:FemaleBALB/cnudemice(6-8weeksold)receivedasubcutaneousinjectionof1×10⁸SKOV3cellsintotherightflank[1].Dosage:2mg/kg,4mg/kgAdministration:Intravenousadministration,every2daysforatotalof12dosesResult:Significantlyinhibitedtumorgrowthcomparedtothecontrol,withTGIvaluesof35.4%,44.3%,respectively.Suggestedafavorablesafetyprofileforthesedosesandschedules.SignificantlydecreasedKi-67expression,amarkerofcellproliferation.REFERENCESYuQ,etal.DiscoveryofNovel4,5-Dihydropyrrolo[3,4-c]pyrazol-6(2H)-one-BasedTubulinInhibitorsTargetingColchicineBindingSitewithPotentAnti-OvarianCancerActivity.JMedChem.2025Oct9;68(19):19908-19932.McePdfHeightC