| CAS NO: | 1700663-41-7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 1700663-41-7 |
| 化学名 | 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 |
| Canonical SMILES | CN(CC1=CNN=C1C2=CC=C(O[C@@H]3C[C@@H](OCCC4CCOCC4)C3)C=C2)CCNC |
| 分子式 | C25H38N4O3 |
| 分子量 | 442.59 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 0.3 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 10 nM 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]. Clinical trial: Up to now, EPZ020411 is still in the preclinical development stage. Reference: |
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