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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Cited by 8 Publications

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.

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) MlnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\xO|IhcA>? Mn3GSG1UVw>? MmjyTWM2OD1zNUi2JOKyKDF5MzDuUS=> MXqyOVc1QTB|NB?=
WT 70 NVHwcpV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LpeFczKGh? NFPiTnFFVVOR NV3kb5RbUUN3ME2yNUDDuSB6IH7N M{\OWVI2PzR7MEO0
G1128S 1022 NIruWGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWC3NkBp M3vmW2ROW09? NXzxWFd6UUN3ME2xNFIhyrFiM{igcm0> NEXENnEzPTd2OUCzOC=>
C1156F 1293 NXf3T3ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXsTotkPzJiaB?= M2THS2ROW09? MVPJR|UxRTJzNzFCtUAyOTVibl2= MUGyOVc1QTB|NB?=
I1171N 519 NYL2ToNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHnO|IhcA>? NUTSfmFZTE2VTx?= MW\JR|UxRTF6NzFCtUA5PyCwTR?= NGjJNHkzPTd2OUCzOC=>
I1171T 445 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTn[5RyPzJiaB?= M{nGUmROW09? MnrNTWM2OD16MjFCtUAyOiCwTR?= NVGyfVl7OjV5NEmwN|Q>
F1174I 184 NEjBTXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TkNlczKGh? MkjkSG1UVw>? MoPkTWM2OD1zMzFCtUAxNjFibl2= M4jkUFI2PzR7MEO0
N1178H 169 NEnEUWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYO3NkBp M3v0T2ROW09? NGLNPG5KSzVyPUSyJOKyKDZibl2= NXvxSG9ROjV5NEmwN|Q>
E1210K 748 MljiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPsXFVkPzJiaB?= MVvEUXNQ NFTIPWdKSzVyPUG4O{DDuSB6NDDuUS=> NVvY[FRiOjV5NEmwN|Q>
C1156F/D1203N 2809 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXa[|NWPzJiaB?= M4jn[mROW09? MVLJR|UxRTJ3NDFCtUA6QSCwTR?= NXP6bYRNOjV5NEmwN|Q>
Ba/F3 NA WT NV7uSpdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUW3NkBp M{W4bWlEPTB;MD6wNlAh|ryP MX:yOVczPzRyMB?=
Ba/F3 NA C1156Y MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\0OVczKGh? MUfJR|UxRTBwMEexJO69VQ>? M3uzeVI2PzJ5NECw
Ba/F3 NA L1196M NEP0ToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13hNVczKGh? NYHlemQxUUN3ME2wMlA1OiEQvF2= NFXGUmozPTd{N{SwNC=>
Ba/F3 NA L1152R NH\jVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTrO|IhcA>? NGnFdZBKSzVyPUCuNlg5KM7:TR?= NUjh[Xc5OjV5Mke0NFA>
Ba/F3 NA G1202R NH;VUFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljxO|IhcA>? MoDPTWM2OD1yLkK3O{DPxE1? Mnj2NlU4Ojd2MEC=
Ba/F3 NA G1269A NV[2PJU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUO3NkBp MlnRTWM2OD1yLkCxPUDPxE1? MYCyOVczPzRyMB?=
Ba/F3 NA S1206Y M{jsTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVO3NkBp MX;JR|UxRTBwMEO3JO69VQ>? NWC1S2VNOjV5Mke0NFA>
Ba/F3 EA WT M{fvO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkT6O|IhcA>? NGXifXpKSzVyPUCuNFIyKM7:TR?= MUKyOVczPzRyMB?=
Ba/F3 EA C1156Y MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTrTJo1PzJiaB?= M3r2PGlEPTB;MD6wNlYh|ryP MVKyOVczPzRyMB?=
Ba/F3 EA L1196M NHHwV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHnO|IhcA>? NXLoRWc{UUN3ME2wMlAyQSEQvF2= M1PyT|I2PzJ5NECw
Ba/F3 EA L1152R NXLWfnN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vwd|czKGh? NF7sSplKSzVyPUCuNFk6KM7:TR?= MXyyOVczPzRyMB?=
Ba/F3 EA G1202R NVnlV49{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\CU3lmPzJiaB?= NWK5epR[UUN3ME2wMlQ3PyEQvF2= M2DZR|I2PzJ5NECw
Ba/F3 EA G1269A M{XoNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm3NkBp MYXJR|UxRTBwMEOzJO69VQ>? MWeyOVczPzRyMB?=
Ba/F3 EA S1206Y NVnIOohJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf1dZpsPzJiaB?= NUXS[HozUUN3ME2wMlA{QCEQvF2= NYrUc3pZOjV5Mke0NFA>

... 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 Recruiting Non-small Cell Lung Cancer Harboring ROS1 Rearrangement Yonsei University July 24 2018 Phase 2
NCT03399487 Recruiting Non-small Cell Lung Cancer Harboring ROS1 Rearrangement Yonsei University July 24 2018 Phase 2
NCT02321501 Recruiting Head and Neck Cancer|Lung Cancer M.D. Anderson Cancer Center|Novartis June 2016 Phase 1
NCT02321501 Recruiting Head and Neck Cancer|Lung Cancer M.D. Anderson Cancer Center|Novartis June 2016 Phase 1
NCT02465528 Completed Tumors With Aberrations in ALK Novartis Pharmaceuticals|Novartis May 6 2016 Phase 2
NCT02465528 Completed Tumors With Aberrations in ALK Novartis Pharmaceuticals|Novartis May 6 2016 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.

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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.

selleck catalog

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

  • Non-specific ALK Inhibitor

    GSK1838705A : IGF-1R, IC50=2.0 nM; IR, IC50=1.6 nM, ALK, IC50=0.5 nM.

  • FDA-approved ALK Inhibitor

    Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).

  • Newest ALK Inhibitor

    ASP3026 New : Novel and selective inhibitor for ALK with IC50 of 3.5 nM.

  • Classic ALK Inhibitor

    TAE684 (NVP-TAE684) : Potent and selective ALK inhibitor with IC50 of 3 nM, 100-fold more sensitive for ALK than InsR.

Related ALK Products4

  • Lorlatinib (PF-6463922) New

    PF-06463922 is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. Phase 1.

  • Erlotinib New

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324) New

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • TAE684 (NVP-TAE684)

    TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR.

  • GSK1838705A

    GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.

    Features:A small-molecule kinase inhibitor of IGF-1R and the insulin receptor.

  • Alectinib (CH5424802)

    Alectinib (CH5424802) is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.

  • AP26113-analog (ALK-IN-1)

    AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.

    Features:At least 10-fold more potent and selective in ALK inhibition relative to crizotinib.

  • ASP3026

    ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.

  • AZD3463

    AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency.

  • Gefitinib (ZD1839)

    Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

    Features:A potent EGFR tyrosine kinase inhibitor.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID