Art. -Nr.: HY-15656A

Ceritinib dihydrochloride

(Synonyms: LDK378 dihydrochloride)

43 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.90%
CAS. Nr.: 1380575-43-8
Formel: C₂₈H₃₈Cl₃N₅O₃S
Molecular Weight:631.06

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ceritinib dihydrochloride Chemical Structure

CAS. Nr.: 1380575-43-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (43)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.2 nM (ALK), 8 nM (IGF-1R), 7 nM (InsR), 23 nM (STK22D)^[1]

In Vitro

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.

In Vivo

Ceritinib dihydrochloride is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. Ceritinib (LDK378) has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. Ceritinib dihydrochloride 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. Ceritinib dihydrochloride induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. Ceritinib (LDK378) shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1380575-43-8
Appearance Solid
Molecular Weight 631.06
Formel C₂₈H₃₈Cl₃N₅O₃S
Color Light yellow to yellow
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
Synonyms

LDK378 dihydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (43)

All Cell Imaging/StainingIn Vivo Efficacy StudyWBCell Proliferation/Viability Assay

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

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.
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.
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.
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

Pulmonary midkine inhibition ameliorates sepsis induced lung injury. [Abstract]

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

Pyrimidine derivatives with antitubercular activity. [Abstract]

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.
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

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

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

Targeting ALK in pediatric RMS does not induce antitumor activity in vivo. [Abstract]

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
bioRxiv

2023 Jul 19.
Patent

US20230158019A1.
Universitat Autònoma de Barcelona

2022 Aug.
Uppsala University

2022 Feb.
Patent

US20200276189A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5846 mL

7.9232 mL

15.8464 mL

5 mM

0.3169 mL

1.5846 mL

3.1693 mL

10 mM

0.1585 mL

0.7923 mL

1.5846 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: PBS

Solubility: 33.33 mg/mL (52.82 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Ceritinib dihydrochloride

43 Cited Publications

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Ceritinib dihydrochloride

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Publications Citing Use of MedChemExpress (MCE) Ceritinib dihydrochloride

Biologische Aktivität

Chemical Information

Publications (43)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ceritinib dihydrochloride Related Classifications

HY-15656A Related Classifications