Ansamitocin-P-3-Antibiotic-C-15003P3-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnsamitocinP-3Cat.No.:HY-15739CASNo.:66584-72-3Synonyms:AntibioticC15003P3;Maytansinolisobutyrate分⼦式:C₃₂H₄₃ClN₂O₉分⼦量:635.14作⽤靶点:Microtubule/Tubulin;ADCCytotoxin;Bacterial;Antibiotic作⽤通路:CellCycle/DNADamage;Cytoskeleton;Antibody-drugConjugate/ADCRelated;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(157.45mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5745mL7.8723mL15.7446mL5mM0.3149mL1.5745mL3.1489mL10mM0.1574mL0.7872mL1.5745mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.94mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(3.94mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.94mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AnsamitocinP-3(AntibioticC15003P3)⼀种微管(microtubule)抑制剂。AnsamitocinP-3⼀种⼤环抗肿瘤抗⽣素。IC50&TargetMaytansinoids体外研究AnsamitocinP-3(AntibioticC15003P3)potentlyinhibitstheproliferationofMCF-7,HeLa,EMT-6/AR1andMDA-MB-231cellsinculturewithahalf-maximalinhibitoryconcentrationof20±3,50±0.5,140±17,and150±1.1pM,respectively.Further,AnsamitocinP3isfoundtobindtopurifiedtubulininvitrowithadissociationconstant(Kd)of1.3±0.7µM.ThebindingofAnsamitocinP3inducesconformationalchangesintubulin.AnsamitocinP3inhibitstheproliferationofMCF-7,HeLa,EMT-6/AR1andMDA-MB-231cellsincultureinaconcentrationdependentmanner.FlowcytometricanalysisofPI-stainedcellssuggeststhatAnsamitocinP3inhibitsthecellcycleprogressionofMCF-7cellsinG2/Mphase.Forexample,26,50and70%ofthecellsarefoundtobeinG2/Mphaseintheabsenceandpresenceof50and100pMAnsamitocinP3,respectively[2].PROTOCOLCellAssay[2]MCF-7,EMT-6/AR1,HeLaandMDA-MB-231cellsareseededin96wellplates.Subsequently,cellsareincubatedwithvehicle(0.1%DMSO)ordifferentconcentrations(1-1000pM)ofAnsamitocinP3for48hinMCF-7cellsand24hforEMT-6/AR1,HeLaandMDA-MB-231cells,respectively.Thehalfmaximalinhibitoryconcentrationofcellproliferation(IC50)forAnsamitocinP3isdeterminedbysulforhodamineBassay.FourindependentexperimentsarecarriedoutinMCF-7cellsandthreeindependentsetsofexperimentsareperformedinEMT-6/AR1,HeLaandMDA-MB-231cells[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JPharmBiomedAnal.2017Jan12;137:170-177.•HealthSciJ.(2021):1-8.•HealthSciJ.(2021):1-7.•HealthScienceJournal.August31,2021.•Chemrxiv.2020Dec.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].KisoT,etal.Screeningformicrotubule-disruptingantifungalagentsbyusingamitotic-arrestmutantofAspergillusnidulansandnovelactionofphenylalaninederivativesaccompanyingtubulinloss.AntimicrobAgentsChemother.2004May;48(5):1739-48[2].VenghateriJB,etal.AnsamitocinP3depolymerizesmicrotubulesandinducesapoptosisbybindingtotubulinatthevinblastinesite.PLoSOne.2013Oct4;8(10):e75182.McePdfHeightCaution: