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| | EPZ020411 Basic information |
| Product Name: | EPZ020411 | | Synonyms: | EPZ020411;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;EPZ020411 HCl;EPZ020411 2HCl;EPZ 020411;EPZ-020411;CS-2262;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]- | | CAS: | 1700663-41-7 | | MF: | C25H38N4O3 | | MW: | 442.59 | | EINECS: | | | Product Categories: | | | Mol File: | 1700663-41-7.mol |  |
| | EPZ020411 Chemical Properties |
| 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 |
| | EPZ020411 Usage And Synthesis |
| 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 | | 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. |
| | EPZ020411 Preparation Products And Raw materials |
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