EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
| パッケージサイズ | 在庫状況 | 単価(税別) |
|---|---|---|
| 2 mg | お問い合わせ | ￥ 25000 |
| 5 mg | お問い合わせ | ￥ 44000 |
| 10 mg | お問い合わせ | ￥ 70500 |
| 25 mg | お問い合わせ | ￥ 147000 |
| 1 mL * 10 mM (in DMSO) | お問い合わせ | ￥ 70500 |
| 説明 | EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM). |
| In vitro | In A375 human melanoma cells exogenously overexpressing PRMT6,treatment with EPZ020411IC50=0.637±0.241 μM) results in a dose-dependent decrease in H3R2 methylation. |
| In vivo | Male Sprague-Dawley rats administered a single dose of EPZ020411 (1 mg/kg by i.v.) ,show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. At dose of EPZ020411(5 mg/kg s.c.) a good bioavailability of 65.6 ± 4.3% is observed, resulting on EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h. |
| 細胞研究 | A375 (CRL-1619) cells are incubated in the presence of increasing concentrations of EPZ020411 up to 20 μM for 48 hours. |
| 動物実験 | Sprague-Dawley rats are treated with EPZ020411(1 mg/kg i.v.) prepared in saline, pH 6.5. |
| 別名 | EPZ020411 2HCl (1700663417(free base)), EPZ020411 2HCl (1700663 41 7(free base)), EPZ-020411 2HCl (1700663-41-7(free base)) |
| 分子量 | 515.51 |
| 分子式 | C25H40Cl2N4O3 |
| CAS No. | T4334 |
Powder: -20°C for 3 years In solvent: -80°C for 2 years
Ethanol: 93 mg/mL (180.4 mM)
DMSO: 93 mg/mL (180.4 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
引用文献
投与量変換You can also refer to dose conversion for different animals. 詳細
In vivo投与量計算 (透明溶液)計算器bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
