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Ceritinib (LDK378) is a selective small molecule inhibitor of ALK, a target found in metastatic non-small cell lung cancer (NSCLC). Ceritinib (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. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib.
Med Oncol. 2022 Dec 28;40(1):64.
FAT4 activation inhibits epithelial-mesenchymal transition (EMT) by promoting autophagy in H2228/Cer cells
LDK378 purchased from AbMole
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Source | Oncotarget (2015). Figure 2. LDK378 |
| Method | p.o. | |
| Cell Lines | nude mice | |
| Concentrations | 25 mg/kg | |
| Incubation Time | 21 day | |
| Results | There was a significant inhibition of tumor growth in the group with a combination of ceritinib and paclitaxel compared with other groups (P < 0.05) |
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Source | Oncotarget (2015). Figure 1. LDK378 |
| Method | MTT assay | |
| Cell Lines | HEK293/ABCB1 and HEK293/ABCG2-R2 cells | |
| Concentrations | 0.5 μM | |
| Incubation Time | 48 h | |
| Results | Based on the cytotoxicity curves, more than 85% of the cells survived at the concentration of 0.5 μM ceritinib |
| Cell Experiment | |
|---|---|
| Cell lines | Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells |
| Preparation 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. |
| Concentrations | ~100 μM |
| Incubation time | 2-3 days |
| Animal Experiment | |
|---|---|
| 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 |
| Molecular Weight | 558.14 |
| Formula | C28H36ClN5O3S |
| CAS Number | 1032900-25-6 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| AP26113 (Brigatinib)
AP26113 (Brigatinib) is a highly potent ALK inhibitor with IC50 of 0.6 nM. |
| X-376
X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitor with IC50 of 0.61 nM. |
| SB431542
SB-431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM). |
| RepSox
RepSox (ALK5 Inhibitor II) is a potent and ATP-competitive inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively). |
| LDN-193189
LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
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