| Field | Specification |
|---|---|
| Alternative names | LDK378 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H36ClN5O3S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Ceritinib (LDK378) is a selective, orally bioavailable, ATP-competitive inhibitor of ALK tyrosine kinase, with an IC50 of 200 pM. It also inhibits IGF-1R, InsR and STK22D, with IC50 values of 8 nM, 7 nM and 23 nM, respectively, and it shows strong antitumor potency[1][2]. It is supplied as a white to off-white solid (C28H36ClN5O3S, MW 558.14) at 99.95% purity.
Physical & Chemical Properties
| CAS Number | 1032900-25-6 |
|---|---|
| Molecular Formula | C28H36ClN5O3S |
| Molecular Weight | 558.14 g/mol |
| Purity | 99.95% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3 |
| Signaling Pathway | Protein Tyrosine Kinase/RTK |
| Solubility | In Vitro: DMSO: 12.5 mg/mL (22.40 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 0.2 nM (ALK), 7 nM (InsR), 8 nM (IGF-1R), 23 nM (STK22D), 60 nM (FLT3), 260 nM (FGFR2)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 12.5 mg/mL (22.40 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 0.5 mg/mL (0.90 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (5.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 0.5 mg/mL (0.90 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (5.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 0.5 mg/mL (0.90 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (5.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Ceritinib additionally inhibits RET (IC50 of 400 nM) and FGFR3 (IC50 of 430 nM), along with 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]. Against ALK enzymatic activity, Ceritinib stays highly potent, with an IC50 value of 200 pM; within a panel of 46 kinases, strong inhibition is seen only for IGF-1R, InsR, and STK22D, with a minimum selectivity of 70-fold. In Ba/F3 cells transfected with a range of kinases, Ceritinib inhibits ALK activity with an IC50 value of 40.7 nM, and the IC50 values against all other kinases tested are >100 nM. Ceritinib (LDK378) displays potent antiproliferative activity, with an IC50 value of 22.8 nM in Karpas 299 cells, a human non-Hodgkin’s Ki-positive large cell lymphoma line carrying the NPM-ALK fusion gene and 26 nM in Ba/F3 cells carrying a transfected NPM-ALK fusion gene. Good selectivity is also seen over wild-type Ba/F3 cells (IC50>2 μM) and over Ba/F3 cells transfected with the Tel-InsR gene (IC50=320 nM)[2].
In Vivo
In rodents and non-rodents, Ceritinib has an excellent pharmacokinetics profile, with an oral bioavailability of >50%. With daily administration, Ceritinib produces dose-dependent tumor growth inhibition and partial tumor regression in the Karpas 299 rat xenograft model, and it can achieve complete tumor regression in the H2228 NSCLC rat xenograft model (carrier of the EML4-ALK fusion gene). Animals tolerate Ceritinib well in both models. Further assessment of the ADME profile of Ceritinib shows relatively good metabolic stability in liver microsomes, modest CYP3A4 inhibition, and some hERG inhibition (IC50 value of 46 μM in hERG patch clamp experiments), but no evidence of QTc prolongation in dog and monkey telemetry studies[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[1]
Conduct in vivo PK studies in mice, rats, dogs, and cynomolgus monkeys. Dose male Balb/c mice with Ceritinib (LDK378) (HCl salt) at 5 mg/kg (n=3) by the intravenous route through the tail vein and at 20 mg/kg (n=3) by the oral route (gavage). Using the same formulation, dose Sprague-Dawley rats with Ceritinib (LDK378) (HCl salt) at 3 mg/kg (n=3) by the intravenous route (tail vein) and at 10 mg/kg (n=3) by the oral route (gavage). Draw blood serially at the scheduled times during the 24 h following dosing. Give male beagle dogs a single dose of Ceritinib (phosphate salt), either intravenous (n=2) as a solution at 5 mg/kg or oral (n=3) as a suspension at 20 mg/kg. Give male cynomolgus monkeys a single dose of Ceritinib (free base), either intravenous (n=2) as a solution at 5 mg/kg or oral (n=3) as a suspension at 60 mg/kg. Draw blood for plasma at prescheduled times during the 144 h after dosing[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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The target landscape of clinical kinase drugs. Science 2017 Dec 1;358(6367):eaan4368.
Targeting the ALK-CDK9-Tyr19 kinase cascade sensitizes ovarian and breast tumors to PARP inhibition via destabilization of the P-TEFb complex. Nat Cancer 2022 Oct;3(10):1211-1227. PMID: 36253486
Molecular landscape, subtypes, and therapeutic vulnerabilities of central nervous system solitary fibrous tumors. Nat Commun 2025 Aug 23;16(1):7870. PMID: 40849425
Targeting NRAS via miR-1304-5p or farnesyltransferase inhibition confers sensitivity to ALK inhibitors in ALK-mutant neuroblastoma. Nat Commun 2024 Apr 23;15(1):3422. PMID: 38653965
Phase separation of EML4-ALK in firing downstream signaling and promoting lung tumorigenesis. Cell Discov 2021 May 11;7(1):33. PMID: 33976114
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med 2018 Jul 18;10(450):eaaq1093.
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. Cell Rep Med 2025 Apr 15;6(4):102053. PMID: 40187357
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. Cell Rep Med 2023 Feb 21;4(2):100911. PMID: 36657446
Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. Pharmacol Res 2025 Nov:221:107993. PMID: 41083089
Integrated clinical, genomic and functional characterization of a novel ALK variant in neuroblastoma. Cancer Lett 2026 May 29:656:218624. PMID: 42217560
