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| | EPZ004777 Basic information |
| Product Name: | EPZ004777 | | Synonyms: | 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;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 EPZ 004777;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;1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran;EPZ004777;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;EPZ004777 (formic acid salt) | | CAS: | 1338466-77-5 | | MF: | C28H41N7O4 | | MW: | 539.67 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1338466-77-5.mol |  |
| | EPZ004777 Chemical Properties |
| 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) |
| | EPZ004777 Usage And Synthesis |
| 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 |
| | EPZ004777 Preparation Products And Raw materials |
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