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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.
In vivio: 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.
| Cell Experiment | |
|---|---|
| Cell lines | KB and KBv200 cells |
| Preparation method | KB and KBv200 cells were treated with 10 μM DOX for 3 h at 37°C, then the cells were washed three times and subsequently maintained at 37°C with culture media without DOX in the presence or absence of 0.5 μM ceritinib at 0, 15, 30, 60 and 120 min, cells were collected and washed three times with ice-cold PBS. |
| Concentrations | 0.5 μM |
| Incubation time | 15, 30, 60 and 120 min |
| Animal Experiment | |
|---|---|
| Animal models | Athymic nude mice |
| Formulation | saline |
| Dosages | 25 mg/kg |
| Administration | p.o. |
| Molecular Weight | 631.06 |
| Formula | C28H38Cl3N5O3S |
| CAS Number | 1380575-43-8 |
| Solubility (25°C) | Water ≥ 100 mg/mL DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Chen J, et al. J Med Chem. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor.
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