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.
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) MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYK3NkBp NHW5WnlFVVOR NYHTdWhDUUN3ME2xOVg3KMLzIEG3N{BvVQ>? MYKyOVc1QTB|NB?=
WT 70 M1O1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfuO|IhcA>? MkLPSG1UVw>? MnvJTWM2OD1{MTFCtUA5KG6P M4TYclI2PzR7MEO0
G1128S 1022 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzacnk4OiCq NGLJeodFVVOR NF7CPXZKSzVyPUGwNkDDuSB|ODDuUS=> MmDhNlU4PDlyM{S=
C1156F 1293 M{P6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXPfms4OiCq NIjUeYVFVVOR M3uzTWlEPTB;MkG3JOKyKDFzNTDuUS=> NEjqUm0zPTd2OUCzOC=>
I1171N 519 NIfnZXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:yOolLPzJiaB?= MUnEUXNQ M{m1cmlEPTB;MUi3JOKyKDh5IH7N MYeyOVc1QTB|NB?=
I1171T 445 NF3qe41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;YSGZqPzJiaB?= MY\EUXNQ NED5eFJKSzVyPUiyJOKyKDF{IH7N NVTwTYFQOjV5NEmwN|Q>
F1174I 184 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIH5OFQ4OiCq M3LtO2ROW09? NH;oOHlKSzVyPUGzJOKyKDBwMTDuUS=> NXjmWnFZOjV5NEmwN|Q>
N1178H 169 M2TwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUT2Z4FLPzJiaB?= MVPEUXNQ NW\YOmFmUUN3ME20NkDDuSB4IH7N NYSx[VlVOjV5NEmwN|Q>
E1210K 748 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLMNGo4OiCq NX;UN3B1TE2VTx?= M2Gx[GlEPTB;MUi3JOKyKDh2IH7N M4O5VVI2PzR7MEO0
C1156F/D1203N 2809 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHQO|IhcA>? M4HsdGROW09? NXLuZW01UUN3ME2yOVQhyrFiOUmgcm0> NE\YXnMzPTd2OUCzOC=>
Ba/F3 NA WT NVvDWYZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUizSXB[PzJiaB?= MkG2TWM2OD1yLkCyNEDPxE1? NIT3eIMzPTd{N{SwNC=>
Ba/F3 NA C1156Y MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX63NkBp M3i4WWlEPTB;MD6wO|Eh|ryP NGiyblUzPTd{N{SwNC=>
Ba/F3 NA L1196M M1y1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu3NkBp NWjWTGVIUUN3ME2wMlA1OiEQvF2= NH3HUo0zPTd{N{SwNC=>
Ba/F3 NA L1152R NVHPN3kyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\WO|IhcA>? MVHJR|UxRTBwMki4JO69VQ>? MlHxNlU4Ojd2MEC=
Ba/F3 NA G1202R NUXjfoNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfYO|IhcA>? MYTJR|UxRTBwMke3JO69VQ>? MlL0NlU4Ojd2MEC=
Ba/F3 NA G1269A MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LHb|czKGh? NGHuPHNKSzVyPUCuNFE6KM7:TR?= MXSyOVczPzRyMB?=
Ba/F3 NA S1206Y NYfteXp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn6ZoFYPzJiaB?= MmW2TWM2OD1yLkCzO{DPxE1? NWjifZkyOjV5Mke0NFA>
Ba/F3 EA WT MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYK3NkBp MlvpTWM2OD1yLkCyNUDPxE1? NEfOfVYzPTd{N{SwNC=>
Ba/F3 EA C1156Y NWLJdXMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPscoFnPzJiaB?= M361UGlEPTB;MD6wNlYh|ryP MnnENlU4Ojd2MEC=
Ba/F3 EA L1196M Mk\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWe3NkBp M{\F[mlEPTB;MD6wNVkh|ryP MXmyOVczPzRyMB?=
Ba/F3 EA L1152R M1rRe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjaSGg4OiCq NIjTOVBKSzVyPUCuNFk6KM7:TR?= M4LFWlI2PzJ5NECw
Ba/F3 EA G1202R M1nrVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzwbIs4OiCq M123W2lEPTB;MD60Olch|ryP MV:yOVczPzRyMB?=
Ba/F3 EA G1269A NGnqenRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXUO|IhcA>? NIrNUnBKSzVyPUCuNFM{KM7:TR?= NYPsTIxXOjV5Mke0NFA>
Ba/F3 EA S1206Y NVzw[ZNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC3NkBp NGPhXW5KSzVyPUCuNFM5KM7:TR?= NEjPe4szPTd{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]

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
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.

Handling Instructions

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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