CPI-169-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemECPI-169Cat.No.:HY-15956ACASNo.:1802175-07-0分?式:C??H??N?O?S分?量:528.66作?靶點(diǎn):HistoneMethyltransferase作?通路:Epigenetics儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(189.16mM)掃描?維碼，*"≥"meanssoluble,butsaturationunknown.運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8916mL9.4579mL18.9157mL5mM0.3783mL1.8916mL3.7832mL10mM0.1892mL0.9458mL1.8916mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(4.73mM);Clearsolution此?案可獲得≥2.5mg/mL(4.73mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.73mM);Clearsolution此?案可獲得≥2.5mg/mL(4.73mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(4.73mM);Clearsolution此?案可獲得≥2.5mg/mL(4.73mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性CPI-169(CPI169R-enantiomer)?種新穎的，有效的EZH2抑制劑，能夠抑制EZH2WT，EZH2Y641N和EZH1的活性，IC50值分別為0.24nM，0.51nM和6.1nM。IC50&TargetEZH2WTEZH2Y641NEZH10.24nM(IC50)0.51nM(IC50)6.1nM(IC50)體外研究CPI-169(CPI169R-enantiomer)inhibitsthecatalyticactivityofPRC2withanIC50of<1nM,decreasescellularlevelsofH3K27me3withanEC50of70nM,andtriggerscellcyclearrestandapoptosisinavarietyofcelllines[1].InKARPAS-422cells,CPI-169showsadose-dependentinhibitoryeffectoncellviability,andproducessynergyanti-proliferativeactivitywhenusedincombinationwithABT-199.In16outof25NHLcelllines,CPI-169alsosuppressescellgrowthwithGI50of<5μM[2].體內(nèi)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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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關(guān)注MCE中國(guó)公眾號(hào)，

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