Filanesib-TFA-ARRY-520-TFA-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFilanesibTFACat.No.:HY-15187BCASNo.:1781834-99-8Synonyms:ARRY-520TFA分?式:C??H??F?N?O?S分?量:534.5作?靶點(diǎn):Kinesin作?通路:CellCycle/DNADamage;Cytoskeleton儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性FilanesibTFA(ARRY-520TFA)?種選擇性的紡錘體驅(qū)動(dòng)蛋?(KSP)抑制劑，對(duì)?KSP作?的IC50值為6nM。FilanesibTFA在體外能誘導(dǎo)?噬導(dǎo)致細(xì)胞死亡。FilanesibTFA具有?效的抗增?活性[1]。IC50&TargetIC50:6nM(KSP)[1]體外研究FilanesibTFAinhibitshumanKSPwithanIC50of6nMbyamechanismdemonstratedtobeuncompetitivewithrespecttoATPandnoncompetitivewithrespecttotubulin[1].FilanesibTFAinducesmitoticarrestinmultiplecelllines[1].FilanesibTFAexhibitsanti-proliferativeagainstabroadrangeofhumanandrodenttumorcelllines[1].FilanesibTFA(0.001-0.1nM;36hours)inducesapoptosis,byamechanismthatisindependentofp53status,asdefinedbyformationofnucleosomesandactivationofcaspases3and7,aswellasaccumulationinSubG0/1byFACS[1].FilanesibTFA(0.1-100nM;18hours)inducestheaccumulationofphospho-HistoneH3(amarkerofmitosis,andanindicatorofmitoticarrest)inHeLacells[1].FilanesibTFA(0.78-6.25nM;44hours)treatmentresultsinG2/Marrest[1].FilanesibTFA(10nM;16hours)treatmentresultsintheformationofmonopolarspindles[1].FilanesibTFApotentlyinducescellcycleblockandsubsequentdeathinleukemiccellsviathemitochondrialpathwayandhaspotentialtoeradicateAMLprogenitorcells[2].FilanesibTFA(3μM;6-24hours)isabletoinducecaspase-2activation[3].FilanesibTFA(0.003-3μM;24-48hours)iscytotoxicinTypeIIEOCcells[3].ApoptosisAnalysis[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:HelacellsConcentration:0.01-0.1nMIncubationTime:36hoursResult:Inducedcelldeathbyapoptosis.CellCycleAnalysis[1]CellLine:HeLacellsConcentration:44hoursIncubationTime:0.78nM,1.56nM,3.13nM,6.25nMResult:ResultedinG2/Marrest.WesternBlotAnalysis[3]CellLine:TypeIIEOCcellsConcentration:3μMIncubationTime:6hours,12hours,24hoursResult:Inducedcaspase-2activationinatime-dependentmanner.CellCytotoxicityAssay[3]CellLine:TypeIIEOCcelllines(A2780,CP70,01-28)Concentration:0.003μM,0.03μM,0.3μM,3μMIncubationTime:24hours,48hoursResult:Effectivelydecreasedcellviabilityinatime-dependentmannerintheTypeIIEOCcelllines.體內(nèi)研究FilanesibTFA(20mg/kg,30mg/kg;i.p.;q4dx3)hasanti-tumoractivitiyinvivo[3].AnimalModel:Femalenudemice,EOCmicexenograftmodel[3]Dosage:20mg/kg,30mg/kgAdministration:Intraperitonealinjection,q4dx3Result:Inducedadecreaseintumorkineticsinadose-dependentmanner.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CancerLett.2021Feb27.?MethodsMolBiol.2018;1711:351-398.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BZCarter,etal.InhibitionofKSPbyARRY-520InducesCellCycleBlockandCellDeathviatheMitochondrialPathwayinAMLCells.[2].KiHyungKim,etal.KSPinhibitorARRY-520asasubstituteforPaclitaxelinTypeIovariancancercells.JTranslMed.2009;7:63.[3].ChristineLemieux,etal.ARRY-520,aNovel,HighlySelectiveKSPInhibitorwithPotentAnti-ProliferativeActivity.AACRAnnualMeeting.2007.McePdfHeightCaution:Producthasnotb