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

Choose Selective ALK Inhibitors

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) NGfCellIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvJU4NTPzJiaB?= NY\lWFFYTE2VTx?= NHrmUIJKSzVyPUG1PFYhyrFiMUezJI5O MlfENlU4PDlyM{S=
WT 70 NF\qR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzBfZI4OiCq MorsSG1UVw>? NUTvWYE6UUN3ME2yNUDDuSB6IH7N M2THV|I2PzR7MEO0
G1128S 1022 M4DpOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2zO|IhcA>? NFrUdIVFVVOR MnnvTWM2OD1zMEKgxtEhOzhibl2= Mnu0NlU4PDlyM{S=
C1156F 1293 MkT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUe3NkBp NXfHclV6TE2VTx?= NHrLUGxKSzVyPUKxO{DDuSBzMUWgcm0> NWHDTm44OjV5NEmwN|Q>
I1171N 519 NGjyV3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjvSJM4OiCq NELhV|NFVVOR MVLJR|UxRTF6NzFCtUA5PyCwTR?= NYi1S4h{OjV5NEmwN|Q>
I1171T 445 NXnSeWFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnmfYg3PzJiaB?= MVrEUXNQ MYXJR|UxRTh{INMxJFEzKG6P Mm\0NlU4PDlyM{S=
F1174I 184 MoL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkf0O|IhcA>? Mlj0SG1UVw>? NHXGXmdKSzVyPUGzJOKyKDBwMTDuUS=> M13DdlI2PzR7MEO0
N1178H 169 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjIbZBzPzJiaB?= NVPsTZpoTE2VTx?= NGj0O2xKSzVyPUSyJOKyKDZibl2= Mkn4NlU4PDlyM{S=
E1210K 748 NVOwOW02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\GO|IhcA>? MnizSG1UVw>? MWnJR|UxRTF6NzFCtUA5PCCwTR?= M3fEeVI2PzR7MEO0
C1156F/D1203N 2809 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XlfFczKGh? M3P0OWROW09? MVnJR|UxRTJ3NDFCtUA6QSCwTR?= M1Pt[VI2PzR7MEO0
Ba/F3 NA WT NVLTelRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rqR|czKGh? NWrSUG9tUUN3ME2wMlAzOCEQvF2= Mor6NlU4Ojd2MEC=
Ba/F3 NA C1156Y MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknEO|IhcA>? NV\tPYVxUUN3ME2wMlA4OSEQvF2= MXOyOVczPzRyMB?=
Ba/F3 NA L1196M MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInSU2M4OiCq MkjMTWM2OD1yLkC0NkDPxE1? NXH1XHVJOjV5Mke0NFA>
Ba/F3 NA L1152R NV\Ke3g2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTUO|IhcA>? MVTJR|UxRTBwMki4JO69VQ>? MYKyOVczPzRyMB?=
Ba/F3 NA G1202R MnnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWi3NkBp NGrMPZlKSzVyPUCuNlc4KM7:TR?= M4HwOVI2PzJ5NECw
Ba/F3 NA G1269A NU\6eVRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXy3NkBp MkTaTWM2OD1yLkCxPUDPxE1? M1PtU|I2PzJ5NECw
Ba/F3 NA S1206Y M3jB[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLUO|IhcA>? MVTJR|UxRTBwMEO3JO69VQ>? MnLBNlU4Ojd2MEC=
Ba/F3 EA WT MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzTSlU4OiCq M4XoT2lEPTB;MD6wNlEh|ryP NGW4TlEzPTd{N{SwNC=>
Ba/F3 EA C1156Y MnTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYm3NkBp NYPQeWRHUUN3ME2wMlAzPiEQvF2= M1vwVlI2PzJ5NECw
Ba/F3 EA L1196M NFfReIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrQO|IhcA>? NHfZenZKSzVyPUCuNFE6KM7:TR?= MoXpNlU4Ojd2MEC=
Ba/F3 EA L1152R M2KxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjSR5gzPzJiaB?= M{ezW2lEPTB;MD6wPVkh|ryP NEO3cHUzPTd{N{SwNC=>
Ba/F3 EA G1202R NFjBdWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrmS2pNPzJiaB?= MVzJR|UxRTBwNE[3JO69VQ>? NGT0cZEzPTd{N{SwNC=>
Ba/F3 EA G1269A MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfyTZo4OiCq NFLrcmhKSzVyPUCuNFM{KM7:TR?= M1nTe|I2PzJ5NECw
Ba/F3 EA S1206Y NYDXeVZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[3NkBp NF7XW3FKSzVyPUCuNFM5KM7:TR?= NIToXmEzPTd{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]
+ 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:[1]
+ 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:[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