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) MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjjRXNZPzJiaB?= M3:0ZWROW09? NGfwSJdKSzVyPUG1PFYhyrFiMUezJI5O M2CwflI2PzR7MEO0
WT 70 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrXcYIxPzJiaB?= M1ywcGROW09? MX3JR|UxRTJzINMxJFghdk1? NFfIS4czPTd2OUCzOC=>
G1128S 1022 Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qwclczKGh? NGLnT3FFVVOR NIDNO4dKSzVyPUGwNkDDuSB|ODDuUS=> MXeyOVc1QTB|NB?=
C1156F 1293 NEjBSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjkO|IhcA>? MmOzSG1UVw>? MUfJR|UxRTJzNzFCtUAyOTVibl2= MVOyOVc1QTB|NB?=
I1171N 519 NXPuS2MxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfTWHc4OiCq MmXKSG1UVw>? MVfJR|UxRTF6NzFCtUA5PyCwTR?= M1jXVFI2PzR7MEO0
I1171T 445 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi3NkBp NW\ZeJhxTE2VTx?= MlX2TWM2OD16MjFCtUAyOiCwTR?= NIL5[GEzPTd2OUCzOC=>
F1174I 184 M37Rd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFroT204OiCq NFfiTXVFVVOR MYTJR|UxRTF|INMxJFAvOSCwTR?= MojINlU4PDlyM{S=
N1178H 169 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe3NkBp M2LMfGROW09? NHq1[GlKSzVyPUSyJOKyKDZibl2= Mnz6NlU4PDlyM{S=
E1210K 748 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPJO|IhcA>? MonxSG1UVw>? NIXCPYpKSzVyPUG4O{DDuSB6NDDuUS=> MmjlNlU4PDlyM{S=
C1156F/D1203N 2809 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XiblczKGh? MUHEUXNQ MkLGTWM2OD1{NUSgxtEhQTlibl2= M2fz[FI2PzR7MEO0
Ba/F3 NA WT M3HLT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\GZ4E4OiCq Ml64TWM2OD1yLkCyNEDPxE1? MXuyOVczPzRyMB?=
Ba/F3 NA C1156Y MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:3NkBp NGXjcWFKSzVyPUCuNFcyKM7:TR?= NIroOHczPTd{N{SwNC=>
Ba/F3 NA L1196M M3ToR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVm3NkBp MVvJR|UxRTBwMESyJO69VQ>? NGPqVXEzPTd{N{SwNC=>
Ba/F3 NA L1152R MmfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjRWZNsPzJiaB?= MX;JR|UxRTBwMki4JO69VQ>? NHT1VIozPTd{N{SwNC=>
Ba/F3 NA G1202R MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\yNpA4OiCq NXK2Ro4xUUN3ME2wMlI4PyEQvF2= MXuyOVczPzRyMB?=
Ba/F3 NA G1269A M4n4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXYe|JEPzJiaB?= M3;CZmlEPTB;MD6wNVkh|ryP M4LBfVI2PzJ5NECw
Ba/F3 NA S1206Y Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYS3NkBp NXHqe29CUUN3ME2wMlA{PyEQvF2= NIruVoczPTd{N{SwNC=>
Ba/F3 EA WT NWK1OGtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW0O|IhcA>? NWfacJJ5UUN3ME2wMlAzOSEQvF2= MUGyOVczPzRyMB?=
Ba/F3 EA C1156Y NHTmNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf1cno4OiCq MV;JR|UxRTBwMEK2JO69VQ>? NVOyZo9iOjV5Mke0NFA>
Ba/F3 EA L1196M NHvKWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGi4c2o4OiCq M4LJfWlEPTB;MD6wNVkh|ryP MYiyOVczPzRyMB?=
Ba/F3 EA L1152R MlXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFy5Oog4OiCq M{HobGlEPTB;MD6wPVkh|ryP M2r4clI2PzJ5NECw
Ba/F3 EA G1202R NWKxcY1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITZ[pQ4OiCq M330cWlEPTB;MD60Olch|ryP MXeyOVczPzRyMB?=
Ba/F3 EA G1269A NEflSY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mni0O|IhcA>? NVe0V3d{UUN3ME2wMlA{OyEQvF2= MYmyOVczPzRyMB?=
Ba/F3 EA S1206Y NYH2VY5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVW3NkBp MV;JR|UxRTBwMEO4JO69VQ>? M2HJNlI2PzJ5NECw

... 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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01828099 Active not recruiting Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis July 9 2013 Phase 3
NCT02040870 Completed Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis March 7 2014 Phase 1|Phase 2
NCT01742286 Recruiting Anaplastic Lymphoma Kinase Novartis Pharmaceuticals|Novartis August 28 2013 Phase 1
NCT01828112 Active not recruiting Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis June 28 2013 Phase 3
NCT01685060 Completed Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis November 26 2012 Phase 2
NCT02450903 Completed Non-Small-Cell Lung Cancer Novartis Pharmaceuticals|Novartis August 21 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