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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2 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.

Purity & Quality Control

Choose Selective ALK Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
STK22D [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
0.2 nM 7 nM 8 nM 23 nM 60 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) NGK0V4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFT1fow4OiCq MYrEUXNQ NHzVTnFKSzVyPUG1PFYhyrFiMUezJI5O M{O1XVI2PzR7MEO0
WT 70 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe3NkBp M2DZRmROW09? MlHzTWM2OD1{MTFCtUA5KG6P NEfxNlczPTd2OUCzOC=>
G1128S 1022 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HpW|czKGh? MYDEUXNQ NUXwN3VlUUN3ME2xNFIhyrFiM{igcm0> MlvHNlU4PDlyM{S=
C1156F 1293 MnP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVG3NkBp M{nrN2ROW09? MVvJR|UxRTJzNzFCtUAyOTVibl2= NYPGOG1wOjV5NEmwN|Q>
I1171N 519 M2m3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC3NkBp NES5NHpFVVOR MWLJR|UxRTF6NzFCtUA5PyCwTR?= MYWyOVc1QTB|NB?=
I1171T 445 M3zBSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWm3NkBp NXfOdHdETE2VTx?= MYLJR|UxRTh{INMxJFEzKG6P NID2boQzPTd2OUCzOC=>
F1174I 184 NW\Jd|hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWW3NkBp MYrEUXNQ Mmn2TWM2OD1zMzFCtUAxNjFibl2= NW\Nb4tUOjV5NEmwN|Q>
N1178H 169 M2Lpfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHieJA4OiCq MVzEUXNQ M2jKb2lEPTB;NEKgxtEhPiCwTR?= NXuzb|h5OjV5NEmwN|Q>
E1210K 748 NHHxVphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVS3NkBp M1;TcWROW09? NV\rTJB5UUN3ME2xPFchyrFiOESgcm0> NV3Kb5pFOjV5NEmwN|Q>
C1156F/D1203N 2809 MmnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV23NkBp MVHEUXNQ MljLTWM2OD1{NUSgxtEhQTlibl2= NVTCbmp3OjV5NEmwN|Q>
Ba/F3 NA WT M1jubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWC3NkBp M3zRR2lEPTB;MD6wNlAh|ryP NWTQW5Y5OjV5Mke0NFA>
Ba/F3 NA C1156Y M{TKdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjheFVWPzJiaB?= MUfJR|UxRTBwMEexJO69VQ>? M4XrXlI2PzJ5NECw
Ba/F3 NA L1196M M4HETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MliwO|IhcA>? MUPJR|UxRTBwMESyJO69VQ>? NFfSb3czPTd{N{SwNC=>
Ba/F3 NA L1152R NWq2eGhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Hz[|czKGh? MW\JR|UxRTBwMki4JO69VQ>? MVKyOVczPzRyMB?=
Ba/F3 NA G1202R NX3lS2dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy2T|BTPzJiaB?= Mo\0TWM2OD1yLkK3O{DPxE1? M2X0W|I2PzJ5NECw
Ba/F3 NA G1269A MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jGTlczKGh? NWLBbGdqUUN3ME2wMlAyQSEQvF2= M1TYO|I2PzJ5NECw
Ba/F3 NA S1206Y MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;3eVczKGh? NGXSRnZKSzVyPUCuNFM4KM7:TR?= M3PYb|I2PzJ5NECw
Ba/F3 EA WT MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrrO|IhcA>? NY\Pems4UUN3ME2wMlAzOSEQvF2= MWGyOVczPzRyMB?=
Ba/F3 EA C1156Y M2i1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWm3NkBp NXj0cWFyUUN3ME2wMlAzPiEQvF2= NGWxcJMzPTd{N{SwNC=>
Ba/F3 EA L1196M Mln2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC0WWVZPzJiaB?= MVLJR|UxRTBwMEG5JO69VQ>? NVjkeYNpOjV5Mke0NFA>
Ba/F3 EA L1152R M1;KbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWS3NkBp NInMVotKSzVyPUCuNFk6KM7:TR?= M4Xoc|I2PzJ5NECw
Ba/F3 EA G1202R MkTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DoNlczKGh? MUfJR|UxRTBwNE[3JO69VQ>? NXSz[nRiOjV5Mke0NFA>
Ba/F3 EA G1269A M3TndWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjYcphqPzJiaB?= MUjJR|UxRTBwMEOzJO69VQ>? NF;qZmQzPTd{N{SwNC=>
Ba/F3 EA S1206Y MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy3NkBp MXjJR|UxRTBwMEO4JO69VQ>? NHzobnkzPTd{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
+ Expand

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
+ Expand
  • 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
+ 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 (35.83 mM) warming
Ethanol 3 mg/mL (5.37 mM)
Water <1 mg/mL

* 1 mg/ml means slightly soluble or 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
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
NCT02336451 Recruiting ALK-positive NSCLC Metastatic to the Brain and/or to Leptomeninges. Novartis Pharmaceuticals|Novartis April 2015 Phase 2
NCT02374489 Recruiting Cholangiocarcinoma National Health Research Institutes, Taiwan|National Cheng-Kung University Hospital|National Taiwan University Hospital March 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