Dot1L-IN-4-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDot1L-IN-4Cat.No.:HY-135127CASNo.:2565705-02-2分?式:C??H??ClF?N?O?S分?量:661.08作?靶點:HistoneMethyltransferase作?通路:Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥220mg/mL(332.79mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5127mL7.5634mL15.1268mL5mM0.3025mL1.5127mL3.0254mL10mM0.1513mL0.7563mL1.5127mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.15mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.15mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.15mM);ClearsolutionBIOLOGICALACTIVITY?物活性Dot1L-IN-4?種有效的類端粒沉默?擾體1(DOT1L)抑制劑，IC50SPADOT1L為0.11nM[1]。IC50&TargetDOT1L0.11nM(IC50)體外研究Dot1L-IN-4(Compound10)istestedincellularassaystoassesstheabilitytoinhibitthedimethylationofH3K79inHeLacells(ED50H3K79me2Elisa=1.7nM)andHOXA9geneexpressioninMolm-13cells(ED50HOXA9RGA=33nM).Dot1L-IN-4alsoinhibitsmixedlineageleukemia(MLL)withanIC50of99μM[1].體內(nèi)研究Dot1L-IN-4(Compound10;300mg/kg;p.o.;qd)isnottoleratedatsuchahighdosebytumorxenograftbearingmice,andata6-foldreduceddose,thetumorgrowthaswellastheHOXA9reportergenemRNAarereducedonlybylessthanhalfascomparedtocontrolanimals[1].AnimalModel:Malemice(C57BL/6)bearingsubcutaneousMV4-11tumorxenografts[1]Dosage:300mg/kg(PharmacokineticAnalysis)Administration:P.o.Result:Wasnottoleratedatsuchahighdosebytumorxenograftbearingmice,andata6-foldreduceddose,thetumorgrowthaswellastheHOXA9reportergenemRNAwerereducedonlybylessthanhalfascomparedtocontrolanimals.REFERENCES[1].FrédéricStauffer,etal.NewPotentDOT1LInhibitorsforinVivoEvaluationinMouse.ACSMed.Chem.Lett.2019,10,12,1655-1660.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr