Tubulin-polymerization-IN-14-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETubulinpolymerization-IN-14Cat.No.:HY-146211CASNo.:2417134-05-3分?式:C??H??ClN?O?分?量:290.74作?靶點:Microtubule/Tubulin;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Tubulinpolymerization-IN-14(Compound20a)?種微管蛋?聚合(tubulinpolymerization)抑制劑，IC50為3.15μM。Tubulinpolymerization-IN-14具有抗?管和抗癌活性，誘導(dǎo)癌細胞凋亡(apoptosis)。IC50&TargetIC50:3.15μM(tubulinpolymerization)[1]體外研究Tubulinpolymerization-IN-14(Compound20a)bindstothecolchicinebindingsiteontubulin[1].Tubulinpolymerization-IN-14(0-1μM;72h)inhibitscancercellgrowth[1].Tubulinpolymerization-IN-14(5-20nM;48h)arrestsK562cellcycleatG2/Mphase,significantlyinducescellapoptosisinK562cellsinaconcentration-dependentmanner,andinducesmitochondrialmembranepotential(MMP)collapseandmitochondrialdysfunctioninK562cells[1].Tubulinpolymerization-IN-14(5-20nM;24h)significantlydecreaseswoundclosureandcapillary-liketubulesformationinaconcentration-dependentmannerinHUVECs[1].CellProliferationAssay[1]CellLine:K562cellsConcentration:0-1μMIncubationTime:72hResult:Showedanti-proliferativeactivitywithanIC50of0.01±0.001μMagainstK562cells.CellCytotoxicityAssay[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:HepG2,HCT-8,MDA-MB-231andHFL-1cellsConcentration:0-1μMIncubationTime:72hResult:ShowedcytotoxicactivitieswithIC50sof0.019±0.002,0.021±0.003,0.02±0.001and0.118±0.007μMagainstHepG2,HCT-8,MDA-MB-231andHFL-1cells,respectively.CellCycleAnalysis[1]CellLine:K562cellsConcentration:5nM,10nMand20nMIncubationTime:48hResult:9.40%,11.54%and15.28%ofcellswerearrestedatG2/Mphaseat5,10and20nM,respectively.ApoptosisAnalysis[1]CellLine:K562cellsConcentration:5nM,10nMand20nMIncubationTime:48hResult:Comparedtothepercentageofapoptosiscellsincontrolgroup(3.25%),thetotalpercentageoftheearly(Annexin-Vt/PI)andlate(Annexin-Vt/PIt)apoptosiscellswere10.46%,48.55%and62.26%afterbeingtreatedat5,10,and20nMfor48h,respectively.CellMigrationAssay[1]CellLine:HUVECsConcentration:5nM,10nMand20nMIncubationTime:24hResult:Afterexposedtocompoundat5,10,and20nMfor24h,cellsmigratedinto67.6%,55.3%and49.2%ofthewoundarea,respectively.體內(nèi)研究Tubulinpolymerization-IN-14(Compound20a)(15and30mg/kg;i.v.;dailyfor21days)displaysobviousanddose-dependentantitumoreffectwithnosignificanttoxicityinthelivertumorallograftmousemodel[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Five-week-oldmaleICRmice,livertumorallograftmodel[1]Dosage:15and30mg/kgAdministration:Intravenousinjection,dailyfor21daysResult:Thedecreaseintumorweightreached68.7%atdosesof30mg/kgperdayat21daysafterinitiationoftreatmentascomparedtovehiclewithoutobviouslossofbodyweight.REFERENCES[1].ShuaiW,etal.Design,synthesisandanticancerpropertiesofisocombretapyridinesaspotentcolchicinebindingsiteinhibitors.EurJMedChem.2020Jul1;197:112308.McePdfHeightCaution:Producthasnotbeenfu