| 產品描述： | ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis |
| 靶點： |
ERK5:0.82 μM (IC50);ERK5 MEF2D:3 μM (IC50);ERK |
| 體內研究： |
ERK5-IN-2 (compound 46) (p.o.; 100?mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin. ERK5-IN-2 (i.v. or p.o.; 10?mg/kg for 0.083-24?hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2?cell permeability assay in both human and mouse. Animal Model: Female CD1 mice (8-10 weeks old) with Matrigel inoculation and female CD1 nude (nu/nu) mice (8-10 weeks old) bearing A2780 human ovarian carcinoma xenografts Dosage: 100?mg/kg Administration: P.o.; twice-daily; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days Result: Tumor volumes were significantly reduced. Animal Model: Female CD1 mice at 8-10 weeks of age Dosage: 10 mg/kg Administration: I.v. or p.o.; 0.083-24?hours Result: The terminal plasma half-life was 38?min, with a plasma clearance of 27?mL/min/kg, and oral bioavailability of 68%. |
| 參考文獻： |
1. Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.576 ml |
12.88 ml |
25.761 ml |
| 5 mM |
0.515 ml |
2.576 ml |
5.152 ml |
| 10 mM |
0.258 ml |
1.288 ml |
2.576 ml |
| 50 mM |
0.052 ml |
0.258 ml |
0.515 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京