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Ceritinib

产品编号 T1791 CAS 1032900-25-6

别名: 色瑞替尼, LDK378

Ceritinib (LDK378) 是一种选择性，具有口服活性的、ATP 竞争性的 ALK 酪氨酸激酶抑制剂，IC50=200 pM。它还抑制 IGF-1R (IC50:8 nM)，InsR (IC50:7 nM) 和 STK22D (IC50:23 nM)。它显示出良好抗肿瘤效力。

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Ceritinib, CAS 1032900-25-6

规格	价格/CNY	货期
5 mg	￥ 397	现货
10 mg	￥ 573	现货
50 mg	￥ 832	现货
100 mg	￥ 1,263	现货
1 mL * 10 mM (in DMSO)	￥ 497	现货

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其他形式的 Ceritinib:

Ceritinib dihydrochloride
现货
Ceritinib D7
询价

选择批次

纯度: 100%

纯度: 99.85%

纯度: 99.46%

纯度: 98.52%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).
靶点活性	ALK:0.2 nM (cell free), STK22D:23 nM (cell free), IGF-1R:8 nM (cell free), Insulin receptor:7 nM (cell free)
体外活性	Ceritinib (LDK378) also inhibits RET (IC50: 400 nM), FGFR3 (IC50: 430 nM), LCK (IC50: 560 nM), JAK2 (IC50: 610 nM), Aurora (IC50: 660 nM), LYN (IC50: 840 nM), EGFR (IC50: 900 nM), and FGFR4 (IC50: 950 nM) [1]. In ALK-positive cell line models, ceritinib was able to effectively inhibit ALK harboring the crizotinib-resistant mutations L1196M, G1269A, I1171T, and S1206Y, but it was ineffective at inhibiting ALK containing the G1202R and F1174C mutations.49 Among a panel of 46 other tested kinases, ceritinib showed strong activity only against IGF-1R (IC50: 8 nM), INSR (IC50: 7 nM), and STK22D (IC50: 23 nM) [2].
体内活性	Mice treated with ceritinib at 50 mg/kg remained in complete remission with no discernible tumor growth for 4 months. In the mice treated with ceritinib at 25 mg/kg, tumor re-growth was observed in 4 out of 8 animals after 1 month, whereas complete remission was maintained in the other 4 animals for 4 months. In a primary explant model derived from a crizotinib-na?ve NSCLC tumor MGH006, treatment with 25 mg/kg ceritinib also led to tumor regressions [3].
激酶实验	All kinases were expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which was produced in E. coli. The kinase activity was measured in the LabChip mobility-shift assay. The assay was performed at 30°C for 60 min. The effect of the compound on the enzymatic activity was obtained from the linear progress curves in the absence and presence of compound and routinely determined from one reading (end point measurement) [1].
细胞实验	Luciferase-expressing cells were incubated with serial dilutions of compounds or DMSO for 2–3 days. Luciferase expression was used as a measure of cell proliferation/survival and was evaluated with the Bright-Glo Luciferase Assay System. IC50 values were generated by using XLFit software [1].
动物实验	SCID beige mice for crizotinib-resistant H2228 xenograft tumor models, nude mice for MGH006 primary explants and MGH045 cells were randomized into groups of 5, 6 or 8 mice with an average tumor volume of ~150 mm^3 and received Crizotinib or ceritinib daily treatments by oral gavage as indicated in each study. Tumor volumes were determined by using caliper measurements and calculated with the formula (Length × Width × Height)/2 [3].

别名	色瑞替尼, LDK378
分子量	558.14
分子式	C28H36ClN5O3S
CAS No.	1032900-25-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 16 mg/mL (28.7 mM)

Ethanol: 3 mg/mL (5.37 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.7917 mL	8.9583 mL	17.9167 mL	44.7916 mL
DMSO / Ethanol	5 mM	0.3583 mL	1.7917 mL	3.5833 mL	8.9583 mL
DMSO	10 mM	0.1792 mL	0.8958 mL	1.7917 mL	4.4792 mL
DMSO	20 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2396 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90. 2. Awad MM, et al. ALK inhibitors in non-small cell lung cancer: crizotinib and beyond. Clin Adv Hematol Oncol. 2014 Jul;12(7):429-39. 3. Friboulet L, et al. The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer. Cancer Discov. 2014 Jun;4(6):662-673. 4. Wang J, Xu X, Wang T, et al. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer[J]. European Journal of Pharmacology. 2021: 173879.

文献引用

1. Wang J, Xu X, Wang T, et al. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer. European Journal of Pharmacology. 2021: 173879. 2. Wang J, Xu X, Wang T, et al. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer. European Journal of Pharmacology. 2021: 173879.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ceritinib 1032900-25-6 Angiogenesis Proteases/Proteasome Tyrosine Kinase/Adaptors Serine Protease IGF-1R ALK 色瑞替尼 Anaplastic lymphoma kinase (ALK) inhibit Insulin Receptor Cluster of differentiation 246 CD246 LDK 378 LDK378 LDK-378 ALK tyrosine kinase receptor Anaplastic lymphoma kinase Inhibitor inhibitor

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Ceritinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords