• 产品描述： Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

• 靶点： ERK2:0.6 nM (IC50);ERK

• 体外研究：
  Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib

• 体内研究：
  Tumor growth inhibition by Tizaterkib ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and Tizaterkib ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and Tizaterkib ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and Tizaterkib ethanesulfonic acid results in a reduction in tumor growth

• 参考文献：
  1. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.022 ml	10.111 ml	20.222 ml
  5 mM	0.404 ml	2.022 ml	4.044 ml
  10 mM	0.202 ml	1.011 ml	2.022 ml
  50 mM	0.04 ml	0.202 ml	0.404 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。

输入产品批号：

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 *