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• 产品描述： Ceritinib (Zykadia, LDK378) dihydrochloride 是一种选择性的、口服可生物利用的、具有ATP竞争性的 ALK 的抑制剂，其IC50值为0.2 nM。Ceritinib dihydrochloride 也抑制 InsR、IGF-1R 和 STK22D，对应的IC50值分别为7 nM、8 nM和23 nM。Ceritinib 具有抗肿瘤活性

• 靶点： ALK(Cell-free assay):0.2 nM; InsR(Cell-free assay):7 nM; IGF-1R(Cell-free assay):8 nM; STK22D(Cell-free assay):23 nM;IGF-1R;ALK

• 体内研究：
  LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg

• 细胞实验： Cell lines: Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells Concentrations: ~100 μM Incubation Time: 2-3 days Method: Luciferase-expressing cells are incubated with serial dilutions of LDK378 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.

• 动物实验： Animal Models: RNU nude rats bearing the Karpas299/H2228 tumors Dosages: ~50 mg/kg Administration: o.g.

• 参考文献：
  1. Thomas H Marsilje, et al. J Med Chem. 2013 Jul 25;56(14):5675-90. 2. Marsilje TH, et al. J Med Chem. 2013, Jun 6.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.585 ml	7.923 ml	15.846 ml
  5 mM	0.317 ml	1.585 ml	3.169 ml
  10 mM	0.158 ml	0.792 ml	1.585 ml
  50 mM	0.032 ml	0.158 ml	0.317 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 *