McMMAF-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEMcMMAFCat.No.:HY-15578CASNo.:863971-19-1分⼦式:C₄₉H₇₆N₆O₁₁分⼦量:925.16作⽤靶点:Drug-LinkerConjugatesforADC;Microtubule/Tubulin作⽤通路:Antibody-drugConjugate/ADCRelated;CellCycle/DNADamage;Cytoskeleton储存⽅式:-20°C,storedundernitrogen*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:≥100mg/mL(108.09mM)扫描⼆维码，*"≥"meanssoluble,butsaturationunknown.运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0809mL5.4045mL10.8089mL5mM0.2162mL1.0809mL2.1618mL10mM0.1081mL0.5404mL1.0809mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。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、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：1%DMSO99%saline2.Solubility:≥0.5mg/mL(0.54mM);Clearsolution请依序添加每种溶剂：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥5mg/mL(5.40mM);Clearsolution1/3www.MedChemEwww.MedChemE此⽅案可获得≥5mg/mL(5.40mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL50.0mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述3.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥5mg/mL(5.40mM);Clearsolution此⽅案可获得≥5mg/mL(5.40mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL50.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性McMMAF由⾼效微管抑制剂MonomethylauristatinF(MMAF)与保护团maleimidocaproyl偶联⽽成。MMAF为抗微管蛋⽩化合物，能通过阻断微管聚合抑制细胞分裂，较MMAE毒性低，可⽤于抗体偶联药物(ADC)。IC50&TargetAuristatin体外研究MMAFisanewauristatinderivativewithachargedC-terminalphenylalaninethatattenuatesitscytotoxicactivitycomparedtoitsunchargedcounterpart,MonomethylauristatinE(MMAE).BecauseofMMAFishighlytoxic,itcannotbeusedasadrugitself.MMAFinducespotentantitumoreffectswhenconjugatedviaproteasecleavablelinkerstoamonoclonalantibodytargetinginternalizing,tumor-specificcellsurfaceantigens.Thelinkertothemonoclonalantibodyisstableinextracellularfluid,butiscleavedbycathepsinoncetheconjugatehasenteredatumorcell,thusactivatingtheanti-mitoticmechanism.户使⽤本产品发表的科研⽂献•JControlRelease.2020Nov10;327:186-197.•Patent.US10087260B2.•Patent.US20160304621A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PolsonAG,etal.Antibody-drugconjugatesforthetreatmentofnon-Hodgkin'slymphoma:targetandlinker-drugselection.CancerRes.2009Mar15;69(6):2358-2364.[2].JianminFang,etal.Anti-her2antibodyandconjugatethereof.US20160304621A1.McePdfHeight2/3www.MedChemEwww.MedChemE关注MCE中国公众号，

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