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Ceritinib

Catalog No. T1791 CAS 1032900-25-6

Synonyms: LDK378

Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).

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Ceritinib, CAS 1032900-25-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 63.00
50 mg	In stock	$ 91.00
100 mg	In stock	$ 136.00
1 mL * 10 mM (in DMSO)	In stock	$ 55.00

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Purity: 100%

Purity: 99.85%

Purity: 99.46%

Purity: 98.52%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).
Targets&IC50	ALK:0.2 nM (cell free), STK22D:23 nM (cell free), IGF-1R:8 nM (cell free), Insulin receptor:7 nM (cell free)
In vitro	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].
In vivo	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].
Kinase Assay	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].
Cell Research	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].
Animal Research	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].

Synonyms	LDK378
Molecular Weight	558.14
Formula	C28H36ClN5O3S
CAS No.	1032900-25-6

Storage

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

Solubility Information

DMSO: 16 mg/mL (28.7 mM)

Ethanol: 3 mg/mL (5.37 mM)

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

References and Literature

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.

Citations

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.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Approved Drug Library Inhibitor Library Membrane Protein-targeted Compound Library Anti-Cancer Active Compound Library

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BMS-363131 3,4 Dichloroisocoumarin Sivelestat PMSF BCX 1470 hydrochloride 2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one Secologanoside ZK824190

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Keywords

Ceritinib 1032900-25-6 Angiogenesis Proteases/Proteasome Tyrosine Kinase/Adaptors Serine Protease IGF-1R ALK 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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