• 产品描述： 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

• 靶点： ERK5:0.82 μM (IC50);ERK5 MEF2D:3 μM (IC50);ERK

• 体内研究：
  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%.

• 参考文献：
  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

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	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：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *