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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3 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.

  • (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.

Purity & Quality Control

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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.
Targets
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) NGXQOIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVG3NkBp MojESG1UVw>? NIjORYVKSzVyPUG1PFYhyrFiMUezJI5O NUjrNXQ6OjV5NEmwN|Q>
WT 70 M1fmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn1b3Q3PzJiaB?= MULEUXNQ NF;jTGJKSzVyPUKxJOKyKDhibl2= NYq5TVNrOjV5NEmwN|Q>
G1128S 1022 MoDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXSyZXFWPzJiaB?= M4HjPWROW09? NUC3WG1yUUN3ME2xNFIhyrFiM{igcm0> M4nUPFI2PzR7MEO0
C1156F 1293 NX\yZmZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jPTVczKGh? NVz5TXRTTE2VTx?= M{nEe2lEPTB;MkG3JOKyKDFzNTDuUS=> MkDMNlU4PDlyM{S=
I1171N 519 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWr0XY9NPzJiaB?= MmXiSG1UVw>? MoqxTWM2OD1zOEegxtEhQDdibl2= NIfMXnMzPTd2OUCzOC=>
I1171T 445 MlrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrKO|IhcA>? M3LaR2ROW09? NIC4bpZKSzVyPUiyJOKyKDF{IH7N NYTSWXY6OjV5NEmwN|Q>
F1174I 184 NV7vcXAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmj3O|IhcA>? M4qzOGROW09? MnT5TWM2OD1zMzFCtUAxNjFibl2= NV7XcpFNOjV5NEmwN|Q>
N1178H 169 MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL1c4k4OiCq MUfEUXNQ MlW2TWM2OD12MjFCtUA3KG6P MW[yOVc1QTB|NB?=
E1210K 748 NVXQW3dvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULGc4xqPzJiaB?= MVTEUXNQ NY\FenBqUUN3ME2xPFchyrFiOESgcm0> MVeyOVc1QTB|NB?=
C1156F/D1203N 2809 NGjX[IZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTiNZk4OiCq NUPXN4ZKTE2VTx?= NGDNTppKSzVyPUK1OEDDuSB7OTDuUS=> M3PsbVI2PzR7MEO0
Ba/F3 NA WT M3izVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXrNJE4OiCq NYTyRXNtUUN3ME2wMlAzOCEQvF2= MmXrNlU4Ojd2MEC=
Ba/F3 NA C1156Y MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVK3NkBp M4fhR2lEPTB;MD6wO|Eh|ryP MVeyOVczPzRyMB?=
Ba/F3 NA L1196M Mm\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVm3NkBp NYLldZhpUUN3ME2wMlA1OiEQvF2= NG\rUWEzPTd{N{SwNC=>
Ba/F3 NA L1152R M3eyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnFco9pPzJiaB?= MkXkTWM2OD1yLkK4PEDPxE1? NEPMXlAzPTd{N{SwNC=>
Ba/F3 NA G1202R MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[3NkBp NUfMdnZ3UUN3ME2wMlI4PyEQvF2= M4PvXVI2PzJ5NECw
Ba/F3 NA G1269A MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEntbGI4OiCq MXLJR|UxRTBwMEG5JO69VQ>? M4rK[FI2PzJ5NECw
Ba/F3 NA S1206Y NE\TfJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DGUlczKGh? MWXJR|UxRTBwMEO3JO69VQ>? Mmr3NlU4Ojd2MEC=
Ba/F3 EA WT MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHJRoc4OiCq NIm3cYZKSzVyPUCuNFIyKM7:TR?= M3nqblI2PzJ5NECw
Ba/F3 EA C1156Y MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWi3NkBp MUDJR|UxRTBwMEK2JO69VQ>? M2fNZVI2PzJ5NECw
Ba/F3 EA L1196M NHvHV3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzRTVc4OiCq NFz0VGVKSzVyPUCuNFE6KM7:TR?= NY\tb3h7OjV5Mke0NFA>
Ba/F3 EA L1152R MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnETFNCPzJiaB?= NWG4eJIxUUN3ME2wMlA6QSEQvF2= NXrJS5NVOjV5Mke0NFA>
Ba/F3 EA G1202R MkH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrmO|IhcA>? M3KwSmlEPTB;MD60Olch|ryP NETVc|IzPTd{N{SwNC=>
Ba/F3 EA G1269A M1XiWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G2fVczKGh? M3vuTGlEPTB;MD6wN|Mh|ryP M4nXVlI2PzJ5NECw
Ba/F3 EA S1206Y NUTrVJRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfHdWp6PzJiaB?= M33XS2lEPTB;MD6wN|gh|ryP NWjCVVJiOjV5Mke0NFA>

... 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]

Protocol

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
Formula

C28H36ClN5O3S

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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 March 2016 Phase 2
NCT02450903 Recruiting Non-Small-Cell Lung Cancer Novartis Pharmaceuticals|Novartis August 2015 Phase 2
NCT02393625 Recruiting ALK-positive NSCLC Novartis Pharmaceuticals|Novartis May 2015 Phase 1
NCT02374489 Recruiting Cholangiocarcinoma National Health Research Institutes, Taiwan|National Cheng-Kung University Hospital|National Taiwan University Hospital March 2015 Phase 2
NCT02276027 Recruiting Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma Novartis Pharmaceuticals|Novartis January 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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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