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 (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
- CBNumber:
- CB94661279
- Molecular Formula:
- C25H39ClN4O3
- Molecular Weight:
- 479.06
- MDL Number:
- MFCD29924736
- MOL File:
- 2070015-25-5.mol
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P305+P351+P338 |
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 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-5501 | EPZ020411(hydrochloride) 98.54% | 2070015-25-5 | 5mg | $150 | 2021-12-16 | Buy |
ChemScene | CS-5501 | EPZ020411(hydrochloride) 98.54% | 2070015-25-5 | 10mg | $250 | 2021-12-16 | Buy |
ChemScene | CS-5501 | EPZ020411(hydrochloride) 98.54% | 2070015-25-5 | 50mg | $650 | 2021-12-16 | Buy |
ChemScene | CS-5501 | EPZ020411(hydrochloride) 98.54% | 2070015-25-5 | 100mg | $1150 | 2021-12-16 | Buy |
Crysdot | CD00005705 | EPZ020411HCl 97% | 2070015-25-5 | 100mg | $1171 | 2021-12-16 | Buy |
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,Uses,Production
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
Target | Value |
PRMT6 (Cell-free assay) | 10 nM |
PRMT1 (Cell-free assay) | 119 nM |
223 nM |
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
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
Chembest Research Laboratories Limited | 021-20908456 | sales@BioChemBest.com | China | 6011 | 61 |
Shanghai Sphchem Co., Ltd. | 21-21-56491756 13512199871 | sales@panhongchem.com | China | 4000 | 55 |
Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7892 | 56 |
BOC Sciences | 16314854226 | info@bocsci.com | United States | 9926 | 65 |
Beijing Solarbio Science & Tecnology Co., Ltd. | 010-50973130 4009686088 | 3193328036@qq.com | China | 29797 | 68 |