| Identification | Back Directory | [Name]
EPZ020411 | [CAS]
1700663-41-7 | [Synonyms]
CS-2262
EPZ020411
EPZ020411 HCl
EPZ020411 2HCl
EPZ 020411;EPZ-020411
N1,N2-dimethyl-N1-((3-(4-((1r,3r)-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine
1,2-Ethanediamine, N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]- | [Molecular Formula]
C25H38N4O3 | [MDL Number]
MFCD28963945 | [MOL File]
1700663-41-7.mol | [Molecular Weight]
442.59 |
| Chemical Properties | Back Directory | [Boiling point ]
619.2±55.0 °C(Predicted) | [density ]
1.16±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
14.53±0.50(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Biological Activity]
epz020411 is an inhibitor of prmt6.prmt6, a member of the protein arginine methyltransferasefamily, comprises 45 enzymes. the post-translational modifications of prmt6 are important regulators of rna processing, transcriptional regulation, and signal transduction. | [in vitro]
in biochemical assays, epz020411 was found to be over 100-fold selective for prmt6/8/1 compared to other histone methyltransferases, such as prmt3, prmt4, prmt5 and prmt7. in addition, epz020411 treatment led to a dose-dependent decrease in h3r2 methylation, while treatment with its prmt6-inactive analog did not generate an ic50 at concentrations up to 20 μm [1]. | [in vivo]
animal study found that male sd rats i.v. administered a single dose of epz020411 at 1 mg/kg showed a moderate clearance of 19.7 ml/min/kg, with a volume of distribution at steady state of 11.1 l/kg, and a mean terminal half-life of 8.54 h. following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 was observed, resulting in epz020411 unbound concentration remaining over the prmt6 ic50 for more than 12 h [1]. | [IC 50]
10 nm | [storage]
Store at -20°C | [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. |
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