1338466-77-5

Basic information

• Product Name: EPZ004777
• Synonyms: 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;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
• CAS NO: 1338466-77-5
• Molecular Formula: C28H41N7O4
• Molecular Weight: 539.66964
• Product Categories: Inhibitors
• Mol File: 1338466-77-5.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 740.7±60.0 °C(Predicted)
• Appearance: /
• Density: 1.33±0.1 g/cm3 (20 oC 760 Torr)
• Solubility: ≥27 mg/mL in DMSO; insoluble in H2O; ≥94.6 mg/mL in EtOH with ultrasonic
• PKA: 12.51±0.70(Predicted)
• CAS DataBase Reference: EPZ004777(CAS DataBase Reference)
• NIST Chemistry Reference: EPZ004777(1338466-77-5)
• EPA Substance Registry System: EPZ004777(1338466-77-5)

Safety Data

• Hazardous Substances Data: 1338466-77-5(Hazardous Substances Data)

Usage

Uses

EPZ 004777 is potent small molecule inhibitor of protein lysine methyltransferase DOT1L.

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].

Upstream product

• 1381761-53-0 1-(4-(tert-butyl)phenyl)-3-(3-oxopropyl)urea 
• 53458-85-8 (2R,3R,4S,5S)-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(chloromethyl)tetrahydrofuran-3,4-diol 
• 69-33-0 tubercidin 

Relevant articles and documents

5'-Deoxidation-5'-isopropyl-substituted-amino nucleoside compound and preparing method and application thereof

The invention discloses a 5'-deoxidation-5'-isopropyl-substituted-amino nucleoside compound shown in a formula 7, a preparing method of the compound shown in the formula 7 and application of the compound shown in the formula 7 to preparing a 5'-deoxidation-5'-polysubstitution amino nucleoside compound 1 as a midbody. The formula is defined in the description.