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

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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) NGe2cFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe3NkBp MoTqSG1UVw>? NUS1d3dFUUN3ME2xOVg3KMLzIEG3N{BvVQ>? MUeyOVc1QTB|NB?=
WT 70 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrzc4Y4OiCq NUjtfmJtTE2VTx?= NUK3UmlZUUN3ME2yNUDDuSB6IH7N MY[yOVc1QTB|NB?=
G1128S 1022 NXnoW|RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nvZ|czKGh? M2nCNWROW09? MofqTWM2OD1zMEKgxtEhOzhibl2= MlzzNlU4PDlyM{S=
C1156F 1293 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j3blczKGh? M{TkR2ROW09? Mke5TWM2OD1{MUegxtEhOTF3IH7N M33pW|I2PzR7MEO0
I1171N 519 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPPOIRJPzJiaB?= MUjEUXNQ NF7MNWxKSzVyPUG4O{DDuSB6NzDuUS=> M2LkWVI2PzR7MEO0
I1171T 445 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[3NkBp MWPEUXNQ MorrTWM2OD16MjFCtUAyOiCwTR?= M2jUN|I2PzR7MEO0
F1174I 184 M3O4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHjXWg4OiCq NWP4V5R2TE2VTx?= MXjJR|UxRTF|INMxJFAvOSCwTR?= MUiyOVc1QTB|NB?=
N1178H 169 MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonEO|IhcA>? Ml\BSG1UVw>? MlrtTWM2OD12MjFCtUA3KG6P MWiyOVc1QTB|NB?=
E1210K 748 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3ubGVCPzJiaB?= MnjSSG1UVw>? NIXiU5pKSzVyPUG4O{DDuSB6NDDuUS=> MmXDNlU4PDlyM{S=
C1156F/D1203N 2809 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XzWFczKGh? M4[2[2ROW09? Mn\qTWM2OD1{NUSgxtEhQTlibl2= Ml3iNlU4PDlyM{S=
Ba/F3 NA WT M3vTXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHniWYk4OiCq MWHJR|UxRTBwMEKwJO69VQ>? NIfpW3UzPTd{N{SwNC=>
Ba/F3 NA C1156Y MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[3NkBp NU\C[XliUUN3ME2wMlA4OSEQvF2= MX:yOVczPzRyMB?=
Ba/F3 NA L1196M MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3iwOFczKGh? M3;ZcWlEPTB;MD6wOFIh|ryP NWjMPW5POjV5Mke0NFA>
Ba/F3 NA L1152R NGrGV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknKO|IhcA>? M3GycmlEPTB;MD6yPFgh|ryP NGrjW5ozPTd{N{SwNC=>
Ba/F3 NA G1202R M2XHOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXB[XA5PzJiaB?= M4DtTmlEPTB;MD6yO|ch|ryP NXfCb4RqOjV5Mke0NFA>
Ba/F3 NA G1269A NWK3NmR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvXNVh5PzJiaB?= NEX5VVlKSzVyPUCuNFE6KM7:TR?= NVjzc5M3OjV5Mke0NFA>
Ba/F3 NA S1206Y NV7ScphqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\RSFczKGh? NUm3[3VVUUN3ME2wMlA{PyEQvF2= Mk\QNlU4Ojd2MEC=
Ba/F3 EA WT Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHkO|IhcA>? NVT3VG0zUUN3ME2wMlAzOSEQvF2= MX[yOVczPzRyMB?=
Ba/F3 EA C1156Y NGLYZWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPkO|IhcA>? NF3qUI5KSzVyPUCuNFI3KM7:TR?= M2\sO|I2PzJ5NECw
Ba/F3 EA L1196M M1W4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\oVWdFPzJiaB?= NYf0[YZLUUN3ME2wMlAyQSEQvF2= MXuyOVczPzRyMB?=
Ba/F3 EA L1152R MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTFXWlmPzJiaB?= M1z5TWlEPTB;MD6wPVkh|ryP MVmyOVczPzRyMB?=
Ba/F3 EA G1202R NXzYOIxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVy3NkBp MmLsTWM2OD1yLkS2O{DPxE1? MmrKNlU4Ojd2MEC=
Ba/F3 EA G1269A Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\OO|IhcA>? MVLJR|UxRTBwMEOzJO69VQ>? NHLMUFIzPTd{N{SwNC=>
Ba/F3 EA S1206Y MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHJb4Q4OiCq Mm\JTWM2OD1yLkCzPEDPxE1? NFXZOW4zPTd{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 (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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID