FR901464-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFR901464Cat.No.:HY-16212CASNo.:146478-72-0分⼦式:C₂₇H₄₁NO₈分⼦量:507.62作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(197.00mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9700mL9.8499mL19.6998mL5mM0.3940mL1.9700mL3.9400mL10mM0.1970mL0.9850mL1.9700mL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、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(4.92mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.92mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FR901464⼀种有效的剪切体(spliceosome)抑制剂，具有显著的抗肿瘤和抗癌作⽤。体外研究FR901464(10-20ng/ml;6-24hours)inhibitsthegrowthofmurinesolidtumors,Colon38carcinomaandMethAfibrosarcoma.FR901464inducescharacteristicG1andG2/MphasearrestinthecellcycleandinternucleosomaldegradationofgenomicDNAwiththesamekineticsasactivationofSV40promoter-dependentcellulartranscriptioninM-8tumorcells[1].FR901464(1-10ng/ml;16hours)suppressesthetranscriptionofsomeinducibleendogenousgenesbutnothousekeepinggenesinM-8cells[1].FR901464exhibitspotentanticanceractivity.ItshowsenhancementofactivityofapromoteroftheSV40DNAtumorvirusat10nMconcentrationinM-8cells[1].REFERENCES[1].HNakajima,etal.Newantitumorsubstances,FR901463,FR901464andFR901465.II.Activitiesagainstexperimentaltumorsinmiceandmechanismofaction.JAntibiot(Tokyo).1996Dec;49(12):1204-11.[2].ArunKGhosh,etal.EnantioselectivetotalsynthesesofFR901464andspliceostatinAandevaluationofsplicingactivityofkeyderivatives.JOrgChem.2014Jun20;79(12):5697-709.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl