CPI-169-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemECPI-169Cat.No.:HY-15956ACASNo.:1802175-07-0分⼦式:C₂₇H₃₆N₄O₅S分⼦量:528.66作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(189.16mM)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1mM1.8916mL9.4579mL18.9157mL5mM0.3783mL1.8916mL3.7832mL10mM0.1892mL0.9458mL1.8916mL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，并请注意储备液的保存⽅式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(4.73mM);Clearsolution此⽅案可获得≥2.5mg/mL(4.73mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。1/3www.MedChemEwww.MedChemE2.请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.73mM);Clearsolution此⽅案可获得≥2.5mg/mL(4.73mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.5mg/mL(4.73mM);Clearsolution此⽅案可获得≥2.5mg/mL(4.73mM，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100μL25.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性CPI-169(CPI169R-enantiomer)⼀种新颖的，有效的EZH2抑制剂，能够抑制EZH2WT，EZH2Y641N和EZH1的活性，IC50值分别为0.24nM，0.51nM和6.1nM。IC50&TargetEZH2WTEZH2Y641NEZH10.24nM(IC50)0.51nM(IC50)6.1nM(IC50)体外研究CPI-169(CPI169R-enantiomer)inhibitsthecatalyticactivityofPRC2withanIC50of<1nM,decreasescellularlevelsofH3K27me3withanEC50of70nM,andtriggerscellcyclearrestandapoptosisinavarietyofcelllines[1].InKARPAS-422cells,CPI-169showsadose-dependentinhibitoryeffectoncellviability,andproducessynergyanti-proliferativeactivitywhenusedincombinationwithABT-199.In16outof25NHLcelllines,CPI-169alsosuppressescellgrowthwithGI50of<5μM[2].体内研究CPI-169(CPI169R-enantiomer)(200mpk,s.c.BID)iswelltoleratedinmicewithnoobservedtoxiceffectorbodyweightloss.CPI-169treatmentleadstotumorgrowthinhibition(TGI)ofanEZH2mutantKARPAS-422DLBCLxenograft.CPI-169(100mpk,BID)withasingledoseofCHOPleadstumorstorapidlyregressandbecomeunpalpable[1].InmicebearingKARPAS-422xenografts,CPI-169(200mg/kg,s.c.)effectivelysuppressesH3K27me3levelsandresultsinlymphomatumorregressionwithoutaffectingbodyweightorcausinganyovertadverseeffects[2].户使⽤本产品发表的科研⽂献•CellSyst.2018Apr25;6(4):424-443.e7.•Patent.US20180263995A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].VidyaBalasubramanian,etal.CPI-169,anovelandpotentEZH2inhibitor,synergizeswithCHOPinvivoandachievescompleteregressioninlymphomaxenograftmodels.CancerResOctober1,201474;16972/3www.MedChemEwww.MedChemE[2].BradleyWD,etal.EZH2inhibitorefficacyinnon-Hodgkin'slymphomadoesnotrequiresuppressionofH3K27monomethylation.ChemBiol.2014Nov20;21(11):1463-75McePdfHeight关注MCE中国公众号，

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