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ChemicalBook--->CAS DataBase List--->2070015-25-5

2070015-25-5

2070015-25-5 Structure

2070015-25-5 Structure
IdentificationBack Directory
[Name]

N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride
[CAS]

2070015-25-5
[Synonyms]

EPZ020411 hydrochloride (EPZ-020411 hydrochloride
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride
[Molecular Formula]

C25H39ClN4O3
[MDL Number]

MFCD29924736
[MOL File]

2070015-25-5.mol
[Molecular Weight]

479.055
Chemical PropertiesBack Directory
[storage temp. ]

Store at 4°C, stored under nitrogen
[solubility ]

DMSO: 50 mg/mL (104.37 mM); Water: ≥ 41 mg/mL (85.58 mM)
[form ]

Solid
[color ]

Off-white to light yellow
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[Biological Activity]

EPZ020411 hydrochloride is a potent and selective small molecule inhibitor of PRMT6 with IC50 of 10 nM.
[in vitro]

EPZ020411 hydrochloride dose-dependently reduced H3R2 methylation in human melanoma A375 cells overexpressing PRMT6 (IC50=0.637±0.241 μM). In biochemical assays, the selectivity of EPZ020411 to PRMT6/8/1 was more than 100-fold higher than that of other histone methyltransferases (including 4 arginine methyltransferases PRMT3, PRMT4, PRMT5, PRMT7). In the parallel artificial membrane permeation test, EPZ020411 has poor permeability.

[in vivo]

EPZ020411 hydrochloride has good bioavailability in rats by subcutaneous injection and is a suitable compound for in vivo studies. After a single intravenous injection of 1 mg/kg EPZ020411 hydrochloride into male Sprague-Dawley rats, its in vivo clearance (CL) was 19.7 ± 1.0 mL/min/kg and its volume of distribution at steady state (Vss) was 11.1 ± 1.6 L/kg, the average half-life was 8.54±1.43 h. Subcutaneous injection of 5 mg/kg has good bioavailability of 65.6 ± 4.3%, and the free concentration of EPZ020411 in the blood is higher than the biochemical IC50 value of PRMT6 for more than 12 hours.
[target]

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> PRMT8
(Cell-free assay)
TargetValue
PRMT6
(Cell-free assay)
10 nM
PRMT1
(Cell-free assay)
119 nM
223 nM
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