• 产品描述： Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor

• 靶点： EGFR;EGFR; BTK

• 体外研究：
  Olmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.In addition, olmutinib at reversal concentration affected neither the protein expression level nor the localization of ABCG2.The results observed from the accumulation/efflux study of olmutinib showed that olmutinib reversed ABCG2-mediated MDR with an increasing intracellular drug accumulation due to inhibited drug efflux.We also had consistent results with the ATPase assay that olmutinib stimulated ATPase activity of ABCG2 up to 3.5-fold.Additionally, the molecular interaction between olmutinib and ABCG2 was identified by docking simulation.Olmutinib not only interacts directly with ABCG2 but also works as a competitive inhibitor of the transport protein

• 参考文献：
  1. Zhang Z , Fu L , Guo X , et al. Olmutinib (HM61713) reversed multidrug resistance by inhibiting the activity of ATPbinding cassette subfamily G member 2 in vitro and in vivo[J]. 2018, 008(004):563-574. 2. Zhang W , Fan Y F , Cai C Y , et al. Olmutinib (BI1482694/HM61713), a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, Reverses ABCG2-Mediated Multidrug Resistance in Cancer Cells[J]. Frontiers in Pharmacology, 2018, 9.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.055 ml	10.276 ml	20.551 ml
  5 mM	0.411 ml	2.055 ml	4.11 ml
  10 mM	0.206 ml	1.028 ml	2.055 ml
  50 mM	0.041 ml	0.206 ml	0.411 ml

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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 *