Ceritinib dihydrochloride
Based on 43 publication(s) in Google Scholar
Ceritinib (LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride shows great antitumor potency.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.90%
- CAS No.: 1380575-43-8
- Formule: C28H38Cl3N5O3S
- Masse moléculaire:631.06
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ceritinib dihydrochloride
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
- Nat Commun. 2025 Aug 23;16(1):7870. [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]
- bioRxiv. 2023 Jul 19.
- Patent. US20230158019A1.
- Universitat Autònoma de Barcelona. 2022 Aug.
- Uppsala University. 2022 Feb.
- Patent. US20200276189A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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WB
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
Activité biologique
IC50: 0.2 nM (ALK), 8 nM (IGF-1R), 7 nM (InsR), 23 nM (STK22D)[1]
Ceritinib dihydrochloride shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1380575-43-8
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Appearance Solid
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Masse moléculaire 631.06
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Formule C28H38Cl3N5O3S
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Color Light yellow to yellow
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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.[H]Cl.[H]Cl
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Synonyms
LDK378 dihydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (43)
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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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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
Molecular landscape, subtypes, and therapeutic vulnerabilities of central nervous system solitary fibrous tumors. [Abstract]2025 Aug 23;16(1):7870. PMID: 40849425 -
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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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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Solvant et solubilité
DMSO : 100 mg/mL (158.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (15.85 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.96 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (52.82 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
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, Jun 6. [Content Brief]
[2]. Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):379-81. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.5846 mL | 7.9232 mL | 15.8464 mL | 39.6159 mL |
| 5 mM | 0.3169 mL | 1.5846 mL | 3.1693 mL | 7.9232 mL | |
| 10 mM | 0.1585 mL | 0.7923 mL | 1.5846 mL | 3.9616 mL | |
| 15 mM | 0.1056 mL | 0.5282 mL | 1.0564 mL | 2.6411 mL | |
| DMSO | 20 mM | 0.0792 mL | 0.3962 mL | 0.7923 mL | 1.9808 mL |
| 25 mM | 0.0634 mL | 0.3169 mL | 0.6339 mL | 1.5846 mL | |
| 30 mM | 0.0528 mL | 0.2641 mL | 0.5282 mL | 1.3205 mL | |
| 40 mM | 0.0396 mL | 0.1981 mL | 0.3962 mL | 0.9904 mL | |
| 50 mM | 0.0317 mL | 0.1585 mL | 0.3169 mL | 0.7923 mL | |
| 60 mM | 0.0264 mL | 0.1321 mL | 0.2641 mL | 0.6603 mL | |
| 80 mM | 0.0198 mL | 0.0990 mL | 0.1981 mL | 0.4952 mL | |
| 100 mM | 0.0158 mL | 0.0792 mL | 0.1585 mL | 0.3962 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ceritinib dihydrochloride Related Classifications
HY-15656A Related Classifications
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