| Identification | More | [Name]
EPZ004777 | [CAS]
1338466-77-5 | [Synonyms]
EPZ004777
7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-
7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
1-(3-((((2R,3S,4R,5R)-5-(4-AMino-7H-pyrrolo[2,3-d]pyriMidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)Methyl)(isopropyl)aMino)propyl)-3-(4-(tert-butyl)phenyl)urea
EPZ 004777
7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine EPZ 004777 | [Molecular Formula]
C28H41N7O4 | [MDL Number]
MFCD25563264 | [MOL File]
1338466-77-5.mol | [Molecular Weight]
539.67 |
| Chemical Properties | Back Directory | [Boiling point ]
740.7±60.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥27 mg/mL in DMSO; insoluble in H2O; ≥94.6 mg/mL in EtOH with ultrasonic | [form ]
solid | [pka]
12.51±0.70(Predicted) |
| Hazard Information | Back Directory | [Uses]
EPZ 004777 is potent small molecule inhibitor of protein lysine methyltransferase DOT1L. | [Definition]
ChEBI: 1-[3-[[(2R,3S,4R,5R)-5-(4-amino-7-pyrrolo[2,3-d]pyrimidinyl)-3,4-dihydroxy-2-oxolanyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea is a N-glycosyl compound. | [Biological Activity]
epz004777 is a specific small-molecule h3k79 methyltransferase dot1l inhibitor that potently inhibits dot1l in a radionuclide homogeneous assay with the half maximal inhibition concentration ic50 value of 400 pm and selectively kills a variety of mll-rearranged leukemia cells, including an mll-af4 leukemia cell line mv4-11 and an mll-af9 leukemia cell line molm13 [1 & 2].epz004777 has also been found to selectively inhibit the proliferation of mll-af10 and calm-af10 transformed cells in a dose dependent manner (ic50: 0.1 μm to 1 μm), in which the mrna expression levels of two hallmark leukemogenic genes (hoxa9 and meis1) are suppressed by epz004777 in a concentration dependent manner [2]. | [storage]
Store at -20°C |
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