Ceritinib mesylate
Based on 41 publication(s) in Google Scholar
Ceritinib (LDK378) mesylate is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib mesylate shows great antitumor potency.
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- CAS No.: 2055376-74-2
- Formule: C30H44ClN5O9S3
- Masse moléculaire:750.35
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Publications Citing Use of MedChemExpress (MCE) Ceritinib mesylate
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
- Nat Commun. 2024 Apr 23;15(1):3422. [Abstract]
- Cell Discov. 2021 May 11;7(1):33. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Pharmacol Res. 2025 Nov:221:107993. [Abstract]
- Cancer Lett. 2026 May 29:656:218624. [Abstract]
- J Transl Med. 2021 Feb 27;19(1):91. [Abstract]
- Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]
- J Med Chem. 2024 Oct 24;67(20):18098-18123. [Abstract]
- Sci Signal. 2015 Dec 8;8(406):ra125. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Eur J Med Chem. 2023 Jan 15:246:114946. [Abstract]
- RSC Adv. 2023 Mar 10;13(12):7929-7938. [Abstract]
- Pharmaceuticals (Basel). 2024 Feb 2;17(2):197. [Abstract]
- Cell Signal. 2022 Apr:92:110264. [Abstract]
- iScience. 2026 Apr 22;29(6):115846. [Abstract]
- Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Antiviral Res. 2026 Jun:250:106417. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867(7):118712. [Abstract]
- AMB Express. 2022 Nov 28;12(1):150. [Abstract]
- J Pharm Pharmacol. 2020 Oct;72(10):1370-1382. [Abstract]
- Analyst. 2025 Dec 1;150(24):5501-5513. [Abstract]
- Toxicol Appl Pharmacol. 2025 Oct:503:117489. [Abstract]
- Toxicol Appl Pharmacol. 2019 Nov 15:383:114781. [Abstract]
- PLoS One. 2025 Jan 21;20(1):e0308747. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Anim Reprod Sci. 2025 Jun:277:107850. [Abstract]
- Cancer Chemother Pharmacol. 2018 Aug;82(2):251-263. [Abstract]
- Cell Physiol Biochem. 2018;45(4):1707-1716. [Abstract]
- Biol Methods Protoc. 2025 Feb 13;10(1):bpaf012. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Xenobiotica. 2018 Oct;48(10):1059-1071. [Abstract]
- Patent. US20230158019A1.
- Universitat Autònoma de Barcelona. 2022 Aug.
- Uppsala University. 2022 Feb.
- Patent. US20200276189A1.
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In Vivo Efficacy Study
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Activité biologique
Description
In Vitro
Ceritinib also inhibits RET (IC50=400 nM), FGFR3 (IC50=430 nM), LCK (IC50=560 nM), JAK2 (IC50=610 nM), Aurora (IC50=660 nM), LYN (50=840 nM), EGFR (IC50=900 nM), and FGFR4 (IC50=950 nM)[1].
Ceritinib retains high potency against the ALK enzymatic activity with an IC50 value of 200 pM and shows only strong inhibition against IGF-1R, InsR, and STK22D out of a panel of 46 kinases with a minimum selectivity of 70-fold. In Ba/F3 cells transfected with various kinases, Ceritinib inhibits ALK activity with an IC50 value of 40.7 nM and had IC50 values of >100 nM against all other kinases tested. Ceritinib shows potent antiproliferative activity with an IC50 value of 22.8 nM in Karpas 299 human non-Hodgkin’s Ki-positive large cell lymphoma carrying the NPM-ALK fusion gene and 26 nM in Ba/F3 cells transfected with the NPM-ALK fusion gene. Ceritinib also shows good selectivity over wild-type Ba/F3 cells (IC50>2 μM) and Ba/F3 cells transfected with Tel-InsR gene (IC50=320 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2055376-74-2
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Masse moléculaire 750.35
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Formule C30H44ClN5O9S3
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SMILES
CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3.CS(=O)(O)=O.CS(=O)(O)=O
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Synonyms
LDK378 mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (41)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Nat Cancer
Targeting the ALK-CDK9-Tyr19 kinase cascade sensitizes ovarian and breast tumors to PARP inhibition via destabilization of the P-TEFb complex. [Abstract]2022 Oct;3(10):1211-1227. PMID: 36253486
Ceritinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
Oral olaparib (50 mg/kg) and ceritinib (7.5 mg/kg), either alone or in combination, five times per week, Tumor volume and Kaplan–Meier survival curves of mice bearing subcutaneous injected SKOV3 ovarian tumors.
Ceritinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
Western blot analysis of indicated proteins in PARPi-sensitive triple-negative breast cancer (TNBC) cells (parental) and TNBC cells with acquired resistance to PARPi (#6 and #15) treated with 50 nM PARPi (talazoparib) or 0.5 µM ALK inhibitor (ALKi; ceritinib), either alone or in combination, for 48 hours.
Ceritinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
Representative images of clonogenic assay results in PARPiresistant ovarian and TNBC cells in the presence of the indicated inhibitor for 12 days. Synergistic inhibition of cell proliferation is defined as CI < 1. CER, ceritinib; OLA, olaparib; Comb, combination of ceritinib and olaparib.
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Nat Commun
Targeting NRAS via miR-1304-5p or farnesyltransferase inhibition confers sensitivity to ALK inhibitors in ALK-mutant neuroblastoma. [Abstract]2024 Apr 23;15(1):3422. PMID: 38653965
Ceritinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Apr 23;15(1):3422. [Abstract]
At 48 h following transfection, the cells were treated with increasing concentrations of ceritinib for 72 h.
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Cell Discov
Phase separation of EML4-ALK in firing downstream signaling and promoting lung tumorigenesis. [Abstract]2021 May 11;7(1):33. PMID: 33976114
Ceritinib mesylate purchased from MedChemExpress. Usage Cited in: Cell Discov. 2021 May 11;7(1):33. [Abstract]
BEAS-2B cells were transfected with GFP–EML4–ALK for 24 h. Cells were treated with DMSO or ALK inhibitors, alectinib (500 nM), ceritinib (500 nM), and GFP fluorescence was monitored through live imaging for up to 12 h.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 15;6(4):102053. PMID: 40187357 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Pharmacol Res
Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]2025 Nov:221:107993. PMID: 41083089 -
Cancer Lett
Integrated clinical, genomic and functional characterization of a novel ALK variant in neuroblastoma. [Abstract]2026 May 29:656:218624. PMID: 42217560 -
J Transl Med
2021 Feb 27;19(1):91. PMID: 33639987 -
Cell Chem Biol
Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation. [Abstract]2018 Aug 16;25(8):996-1005.e4. PMID: 29909991 -
J Med Chem
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations. [Abstract]2024 Oct 24;67(20):18098-18123. PMID: 39361251 -
Sci Signal
Pleiotrophin promotes vascular abnormalization in gliomas and correlates with poor survival in patients with astrocytomas. [Abstract]2015 Dec 8;8(406):ra125. PMID: 26645582 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Eur J Med Chem
2023 Jan 15:246:114946. PMID: 36459759 -
RSC Adv
Development and validation of an UPLC-ESI-MS/MS method for quantification of duvelisib in plasma: application to pharmacokinetic study in rats. [Abstract]2023 Mar 10;13(12):7929-7938. PMID: 36909770 -
Pharmaceuticals (Basel)
Therapeutic Implications of Ceritinib in Cholangiocarcinoma beyond ALK Expression and Mutation. [Abstract]2024 Feb 2;17(2):197. PMID: 38399413 -
Cell Signal
EML4-ALK G1202R mutation induces EMT and confers resistance to ceritinib in NSCLC cells via activation of STAT3/Slug signaling. [Abstract]2022 Apr:92:110264. PMID: 35085771 -
iScience
Ceritinib induces ferroptosis via TRIM21-mediated GLUT1 ubiquitination and AMPK-driven metabolic reprogramming in breast cancer. [Abstract]2026 Apr 22;29(6):115846. PMID: 42181273 -
Mol Oncol
Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. [Abstract]2017 Aug;11(8):996-1006. PMID: 28432815
Ceritinib mesylate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]
Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.
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Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Antiviral Res
Repurposing screen using a robust human rhinovirus infectious clone identifies pyrvinium pamoate with antiviral activity. [Abstract]2026 Jun:250:106417. PMID: 42025967 -
Biochim Biophys Acta Mol Cell Res
ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. [Abstract]2020 Jul;1867(7):118712. PMID: 32224191 -
AMB Express
Insights into the antimicrobial effects of ceritinib against Staphylococcus aureus in vitro and in vivo by cell membrane disruption. [Abstract]2022 Nov 28;12(1):150. PMID: 36443539 -
J Pharm Pharmacol
1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-3-(2-(dimethylamino)ethyl)imidazolidin-2-one (ZX-42), a novel ALK inhibitor, induces apoptosis and protective autophagy in H2228 cells. [Abstract]2020 Oct;72(10):1370-1382. PMID: 32596809 -
Analyst
Determination of veliparib metabolic stability in the human liver microsomes using a hydrophilic interaction UPLC-MS/MS quantitative method: greenness assessment with an in silico study for ADME, DEREK alarms and metabolic lability. [Abstract]2025 Dec 1;150(24):5501-5513. PMID: 41231074 -
Toxicol Appl Pharmacol
Ceritinib (LDK378) inhibits laryngeal squamous cell carcinoma progression via regulating ROS-induced mitochondrial apoptosis and inducing oxidative stress. [Abstract]2025 Oct:503:117489. PMID: 40744212 -
Toxicol Appl Pharmacol
A novel ALK inhibitor ZYY inhibits Karpas299 cell growth in vitro and in a mouse xenograft model and induces protective autophagy. [Abstract]2019 Nov 15:383:114781. PMID: 31618659 -
PLoS One
Inhibition of the anti-apoptotic protein BCL2 in EML4-ALK cell models as a second proposed therapeutic target for non-small cell lung cancer. [Abstract]2025 Jan 21;20(1):e0308747. PMID: 39836700 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Anim Reprod Sci
Differential impact of the kinase inhibitors ruxolitinib and ceritinib on porcine sperm in vitro. [Abstract]2025 Jun:277:107850. PMID: 40318512 -
Cancer Chemother Pharmacol
2018 Aug;82(2):251-263. PMID: 29855693 -
Cell Physiol Biochem
Inhibition of Collagen Related Peptide Induced Platelet Activation and Apoptosis by Ceritinib. [Abstract]2018;45(4):1707-1716. PMID: 29490295 -
Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Xenobiotica
Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]2018 Oct;48(10):1059-1071. PMID: 29034773 -
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Pureté et documentation
Références
[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. [Content Brief]
[2]. Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ceritinib mesylate Related Classifications
HY-15656B Related Classifications
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