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) M2jGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS3NkBp NFXZV4VFVVOR MXvJR|UxRTF3OE[gxtEhOTd|IH7N M4HROlI2PzR7MEO0
WT 70 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33kPFczKGh? NX3QZ3YyTE2VTx?= M{DpdWlEPTB;MkGgxtEhQCCwTR?= NHHmO28zPTd2OUCzOC=>
G1128S 1022 Mnv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWOz[GN[PzJiaB?= MYLEUXNQ MYHJR|UxRTFyMjFCtUA{QCCwTR?= M3jvSVI2PzR7MEO0
C1156F 1293 NV7MNpU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVK3NkBp NFzRU25FVVOR MnvtTWM2OD1{MUegxtEhOTF3IH7N NVvwSnBrOjV5NEmwN|Q>
I1171N 519 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PtUVczKGh? MYXEUXNQ M2jBdWlEPTB;MUi3JOKyKDh5IH7N NE\1blIzPTd2OUCzOC=>
I1171T 445 NXn1c|VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;SO|IhcA>? MkPISG1UVw>? MXHJR|UxRTh{INMxJFEzKG6P Mo\2NlU4PDlyM{S=
F1174I 184 Ml3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvXXGRwPzJiaB?= MUnEUXNQ NGTzXm5KSzVyPUGzJOKyKDBwMTDuUS=> NHXjdVUzPTd2OUCzOC=>
N1178H 169 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zMNFczKGh? NVzIe|BoTE2VTx?= MXzJR|UxRTR{INMxJFYhdk1? NHjiR|AzPTd2OUCzOC=>
E1210K 748 M1jUVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\5O|IhcA>? MmXBSG1UVw>? M4\ETmlEPTB;MUi3JOKyKDh2IH7N NWCye4lJOjV5NEmwN|Q>
C1156F/D1203N 2809 MoT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TFb|czKGh? MUPEUXNQ M3\TV2lEPTB;MkW0JOKyKDl7IH7N NGLCe5kzPTd2OUCzOC=>
Ba/F3 NA WT MnnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fVUFczKGh? M2\iRmlEPTB;MD6wNlAh|ryP MYKyOVczPzRyMB?=
Ba/F3 NA C1156Y NFzl[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PURlczKGh? NE\oVVVKSzVyPUCuNFcyKM7:TR?= MXuyOVczPzRyMB?=
Ba/F3 NA L1196M NYnnOVg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDYOGU4OiCq NFHuS3RKSzVyPUCuNFQzKM7:TR?= NXfz[Y5jOjV5Mke0NFA>
Ba/F3 NA L1152R MkXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTOO|IhcA>? NIqyfmVKSzVyPUCuNlg5KM7:TR?= MofRNlU4Ojd2MEC=
Ba/F3 NA G1202R NHf3T|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL0XYM4OiCq MUXJR|UxRTBwMke3JO69VQ>? M{HVblI2PzJ5NECw
Ba/F3 NA G1269A M2fPbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjsZ3BxPzJiaB?= M3\5SWlEPTB;MD6wNVkh|ryP M4fRRlI2PzJ5NECw
Ba/F3 NA S1206Y NFL5RoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWm3NkBp Mn3qTWM2OD1yLkCzO{DPxE1? NUnnNmFiOjV5Mke0NFA>
Ba/F3 EA WT MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETONY84OiCq MXLJR|UxRTBwMEKxJO69VQ>? NEjKeoMzPTd{N{SwNC=>
Ba/F3 EA C1156Y M3fYN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi0cJU4OiCq MW\JR|UxRTBwMEK2JO69VQ>? NGfXOZUzPTd{N{SwNC=>
Ba/F3 EA L1196M MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfwfmg4OiCq MVXJR|UxRTBwMEG5JO69VQ>? NF3acpkzPTd{N{SwNC=>
Ba/F3 EA L1152R MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLNO|IhcA>? MkHMTWM2OD1yLkC5PUDPxE1? MXmyOVczPzRyMB?=
Ba/F3 EA G1202R M3[1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGe0Olc4OiCq MVzJR|UxRTBwNE[3JO69VQ>? Mlf2NlU4Ojd2MEC=
Ba/F3 EA G1269A MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;ZWWNxPzJiaB?= M2DtN2lEPTB;MD6wN|Mh|ryP NYq5T4Z1OjV5Mke0NFA>
Ba/F3 EA S1206Y NX65OHYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT1WndiPzJiaB?= MlXxTWM2OD1yLkCzPEDPxE1? MXqyOVczPzRyMB?=

... 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