BiologicalActivity
HighlypotentDOT1Linhibitor(IC50=0.4nM).Exhibits>1000-foldselectivityforDOT1Loverapanelofothermethyltransferases.SelectivelyinhibitsproliferationandinducesapoptosisofMLL-rearrangedcellsinvitro.ProlongssurvivalinaMLLxenograftmousemodel.
LicensingInformation
SoldunderlicensefromEpizyme,Inc.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofEPZ004777isreviewedonthechemicalprobeswebsite.
TechnicalData
| M.Wt | 539.67 |
| Formula | C28H41N7O4 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1338466-77-5 |
| PubChemID | 56962336 |
| InChIKey | WXRGFPHDRFQODR-ICLZECGLSA-N |
| Smiles | NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3)C=C2)=NC=N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.97 | 100 | |
| ethanol | 53.97 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight539.67.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.85mL | 9.26mL | 18.53mL |
| 5mM | 0.37mL | 1.85mL | 3.71mL |
| 10mM | 0.19mL | 0.93mL | 1.85mL |
| 50mM | 0.04mL | 0.19mL | 0.37mL |
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