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• 產(chǎn)品描述： Ceritinib (Zykadia, LDK378) dihydrochloride 是一種選擇性的、口服可生物利用的、具有ATP競爭性的 ALK 的抑制劑，其IC50值為0.2 nM。Ceritinib dihydrochloride 也抑制 InsR、IGF-1R 和 STK22D，對應的IC50值分別為7 nM、8 nM和23 nM。Ceritinib 具有抗腫瘤活性

• 靶點： 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

• 體內研究：
  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

• 細胞實驗： 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.

• 動物實驗： Animal Models: RNU nude rats bearing the Karpas299/H2228 tumors Dosages: ~50 mg/kg Administration: o.g.

• 參考文獻：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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：部分產(chǎn)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。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系，公式為：

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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