ChemicalBook > CAS DataBase List > 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

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

Product 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 No.
2070015-25-5
Chemical 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
Synonyms
EPZ020411 hydrochloride, 10 mM in DMSO;EPZ020411 hydrochloride (EPZ-020411 hydrochloride;N1,N2-Dimethyl-N1-((3-(4-(trans-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine 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
CBNumber
CB94661279
Molecular Formula
C25H39ClN4O3
Formula Weight
479.06
MOL File
2070015-25-5.mol
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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 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-5501
Product name
EPZ020411(hydrochloride)
Purity
98.54%
Packaging
5mg
Price
$150
Updated
2021/12/16
ChemScene
Product number
CS-5501
Product name
EPZ020411(hydrochloride)
Purity
98.54%
Packaging
10mg
Price
$250
Updated
2021/12/16
ChemScene
Product number
CS-5501
Product name
EPZ020411(hydrochloride)
Purity
98.54%
Packaging
50mg
Price
$650
Updated
2021/12/16
ChemScene
Product number
CS-5501
Product name
EPZ020411(hydrochloride)
Purity
98.54%
Packaging
100mg
Price
$1150
Updated
2021/12/16
Crysdot
Product number
CD00005705
Product name
EPZ020411HCl
Purity
97%
Packaging
100mg
Price
$1171
Updated
2021/12/16
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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 Chemical Properties,Usage,Production

Uses

EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer[1][2].

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

IC 50

PRMT6: 0.01 μM (IC50); PRMT1: 0.119 μM (IC50); PRMT8: 0.223 μM (IC50)

References

[1] Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659. DOI:10.1021/acsmedchemlett.5b00071
[2] He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020 Jan 1;10(1):133-150. DOI:10.7150/thno.37362

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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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 Suppliers

China 33 United States 5 Global 38
Chembest Research Laboratories Limited
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TargetMol Chemicals Inc.
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2070015-25-5, 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 hydrochlorideRelated Search:


  • 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
  • EPZ020411 hydrochloride (EPZ-020411 hydrochloride
  • N1,N2-Dimethyl-N1-((3-(4-(trans-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine hydrochloride
  • EPZ020411 hydrochloride, 10 mM in DMSO
  • 2070015-25-5