Ceritinib (LDK378)

Catalog No.S7083

Ceritinib (LDK378) Chemical Structure

Molecular Weight(MW): 558.14

Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.

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5 Customer Reviews

  • Quantitation of crystal violet uptake by ORF-expressing cells exposed to crizotinib (CRZ) or ceritinib (CER) normalized to Lac Z. Mean and SE are shown for six (CRZ) or four (CER) independent experiments of three replicates each.

    Cancer Cell, 2015, 27(3): 397-408 . Ceritinib (LDK378) purchased from Selleck.

    H3122 cells expressing pRS or shSMARCE1 vectors were cultured in the absence or presence of 100 nM NVP-TAE684, 400 nM Ceritinib, 1 μM gefitinib or their combination for 3 h. Cell lysates were harvested for immunoblot analysis and probed for the indicated proteins.

    Cell Res, 2015, 25(4): 445-58. Ceritinib (LDK378) purchased from Selleck.

  • Immunoblot of BEAS-2B/LacZ and BEAS-2B/EA samples treated with serially diluted concentration of crizotinib (CZT) and ceritinib (CER; 0, 0.01, 0.1, 0.5, and 1 μmol/L) for 48 hours. Results are shown as means ± SD (N=3).

    Clin Cancer Res, 2018, doi:10.1158/1078-0432. Ceritinib (LDK378) purchased from Selleck.

    Immunoblots of integrin b3 expression in H3122 and H2228 cells treated with DMSO (0 mmol/L), 1 mmol/L crizotinib (CZT), or 1 mmol/L ceritinib (CER) for 48 hours.

    Clin Cancer Res, 2018, 24(17):4162-4174. Ceritinib (LDK378) purchased from Selleck.

  • (A) H3122 LDK_R show increased invasive and migratory capabilities compared to parental H3122, (B) loss of E-cadherin and increased mesenchymal markers including vimentin and AXL. Knockdown of vimentin decreased AXL expression in H3122 LDK_R.

    Mol Oncol, 2016, 10(4):601-9. Ceritinib (LDK378) purchased from Selleck.

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Biological Activity

Description Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.
Features Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
ALK [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
0.2 nM 7 nM 8 nM
In vitro

LDK378 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Parental(+IL3) NGj6N5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjlO4w4OiCq NYKyVnBXTE2VTx?= NYHEUGFqUUN3ME2xOVg3KMLzIEG3N{BvVQ>? NG\ublgzPTd2OUCzOC=>
WT 70 NHj1cWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUG3NkBp MVfEUXNQ MX;JR|UxRTJzINMxJFghdk1? M{X6bFI2PzR7MEO0
G1128S 1022 MlzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzYWnJCPzJiaB?= NVi4enBnTE2VTx?= M1PjNWlEPTB;MUCyJOKyKDN6IH7N MkHFNlU4PDlyM{S=
C1156F 1293 NIKxNolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XpPFczKGh? MnW5SG1UVw>? NEnIW2ZKSzVyPUKxO{DDuSBzMUWgcm0> M1f0PFI2PzR7MEO0
I1171N 519 Mmj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nzOlczKGh? MlLsSG1UVw>? NV\ZWWdnUUN3ME2xPFchyrFiOEegcm0> NIq2V2czPTd2OUCzOC=>
I1171T 445 M3Xuc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXq3NkBp NX7ZVVE1TE2VTx?= MoHtTWM2OD16MjFCtUAyOiCwTR?= MYmyOVc1QTB|NB?=
F1174I 184 M3joNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{KwU|czKGh? MU\EUXNQ MoqyTWM2OD1zMzFCtUAxNjFibl2= MoHNNlU4PDlyM{S=
N1178H 169 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Tu[lczKGh? M{XWU2ROW09? NHjKSWdKSzVyPUSyJOKyKDZibl2= NW\HWHNJOjV5NEmwN|Q>
E1210K 748 NELzV4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH3VWxrPzJiaB?= M3\0OmROW09? M3Syc2lEPTB;MUi3JOKyKDh2IH7N M3T4VFI2PzR7MEO0
C1156F/D1203N 2809 MlzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;vWYd4PzJiaB?= NXr3PVRFTE2VTx?= NIq1OYpKSzVyPUK1OEDDuSB7OTDuUS=> M2iycFI2PzR7MEO0
Ba/F3 NA WT MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2raSlczKGh? NI\HflZKSzVyPUCuNFIxKM7:TR?= MoT5NlU4Ojd2MEC=
Ba/F3 NA C1156Y NHG2Z4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUG3NkBp M2W1PWlEPTB;MD6wO|Eh|ryP MnHLNlU4Ojd2MEC=
Ba/F3 NA L1196M NFj2ZpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTlSpJCPzJiaB?= NYrIe|NoUUN3ME2wMlA1OiEQvF2= M2DJSlI2PzJ5NECw
Ba/F3 NA L1152R M4HRV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXQ[ZMyPzJiaB?= NH\CbVNKSzVyPUCuNlg5KM7:TR?= NGLEZnozPTd{N{SwNC=>
Ba/F3 NA G1202R M4nEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTlXok4OiCq MXrJR|UxRTBwMke3JO69VQ>? NVPpdJZvOjV5Mke0NFA>
Ba/F3 NA G1269A MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS3O|IhcA>? MUPJR|UxRTBwMEG5JO69VQ>? M1nL[FI2PzJ5NECw
Ba/F3 NA S1206Y NEG4TmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3Fb3M4OiCq M4nWTGlEPTB;MD6wN|ch|ryP M1jLbFI2PzJ5NECw
Ba/F3 EA WT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXTO|IhcA>? MWDJR|UxRTBwMEKxJO69VQ>? NVG1bXJ4OjV5Mke0NFA>
Ba/F3 EA C1156Y NV3uV3pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;1PFczKGh? M1\TPWlEPTB;MD6wNlYh|ryP NFzLVZQzPTd{N{SwNC=>
Ba/F3 EA L1196M M{X1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL0V4c4OiCq Ml\DTWM2OD1yLkCxPUDPxE1? NUfuPHpkOjV5Mke0NFA>
Ba/F3 EA L1152R MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;OUGc4OiCq NHjYcopKSzVyPUCuNFk6KM7:TR?= MW[yOVczPzRyMB?=
Ba/F3 EA G1202R NFH0[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NECwWVY4OiCq M1roW2lEPTB;MD60Olch|ryP M4r3VVI2PzJ5NECw
Ba/F3 EA G1269A NIr0TWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUO5R49oPzJiaB?= NIXTWXBKSzVyPUCuNFM{KM7:TR?= Ml7rNlU4Ojd2MEC=
Ba/F3 EA S1206Y NFn1bJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1mxblczKGh? MoHiTWM2OD1yLkCzPEDPxE1? NFTpdVIzPTd{N{SwNC=>

... Click to View More Cell Line Experimental Data

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


Kinase Assay:[1]
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Enzymatic kinase profiling description:

All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of LDK378 on the enzymatic activity is obtained from the linear progress curves in the absence and presence of LDK378 and routinely determines from one reading (end point measurement)
Cell Research:[1]
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  • Cell lines: Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells
  • Concentrations: ~100 μM
  • Incubation Time: 2-3 days
  • Method: Luciferase-expressing cells are incubated with serial dilutions of LDK378 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: RNU nude rats bearing the Karpas299/H2228 tumors
  • Formulation: LDK378 (phosphate salt) formulated in 0.5% methylcellulose/0.5% Tween 80
  • Dosages: ~50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL warmed (35.83 mM)
Ethanol 3 mg/mL (5.37 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 558.14


CAS No. 1032900-25-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03399487 Not yet recruiting Non-small Cell Lung Cancer Harboring ROS1 Rearrangement Yonsei University January 2018 Phase 2
NCT02321501 Recruiting Head and Neck Cancer|Lung Cancer M.D. Anderson Cancer Center|Novartis June 2016 Phase 1
NCT02465528 Recruiting Tumors With Aberrations in ALK Novartis Pharmaceuticals|Novartis May 6 2016 Phase 2
NCT02450903 Completed Non-Small-Cell Lung Cancer Novartis Pharmaceuticals|Novartis August 21 2015 Phase 2
NCT02393625 Recruiting ALK-positive NSCLC Novartis Pharmaceuticals|Novartis May 27 2015 Phase 1
NCT02336451 Recruiting ALK-positive Non-small Cell Lung Cancer Novartis Pharmaceuticals|Novartis April 1 2015 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    how to reconstitute the inhibitor for oral administration to mice?

  • Answer:

    You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID