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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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.
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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.
|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.|
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. 
|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. |
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)
|In vitro||DMSO||20 mg/mL (35.83 mM) warming|
|Ethanol||3 mg/mL (5.37 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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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|
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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