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CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 induced concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells, and displayed dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice. CEP-28122 displayed marginal antitumor activity against ALK-negative human tumor xenografts under the same dosing regimens. Administration of CEP-28122 was well tolerated in mice and rats. In summary, CEP-28122 is a highly potent and selective orally active ALK inhibitor with a favorable pharmaceutical and pharmacokinetic profile and robust and selective pharmacologic efficacy against ALK-positive human cancer cells and tumor xenograft models in mice.
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Source | Mol Cancer Ther (2012). Figure 2. CEP-28122 |
| Method | MTS assays | |
| Cell Lines | NPM-ALK–positive ALCL (Karpas-299 and Sup-M2) cells | |
| Concentrations | 30, 100, 300 and 1,000 nmol/L | |
| Incubation Time | 48 h | |
| Results | The activity of growth inhibition and caspase activation are consistent with the cellular inhibition of NPM-ALK phosphorylation. In contrast, CEP-28122 had no-to-marginal growth inhibition and did not induce significant caspase 3/7 activation in ALK-negative leukemia Toledo and lymphoma HuT-102 cells at concentrations up to 3,000 nmol/L |
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Source | Mol Cancer Ther (2012). Figure 1. CEP-28122 |
| Method | immunoblot analysis | |
| Cell Lines | NSCLC NCI-H2228 and NCI-H3122 cells | |
| Concentrations | 30, 100, 300 and 1,000 nmol/L | |
| Incubation Time | 2 h | |
| Results | In a cellular phosphorylation assay, treatment of NPMALK–positive ALCL cells, Sup-M2 and Karpas-299, with CEP-28122 led to concentration-related inhibition of NPM-ALK tyrosine (664) phosphorylation, with calculated cellular IC50 values of 20 to 30 nmol/L |
| Cell Experiment | |
|---|---|
| Cell lines | NPM-ALK–positive ALCL (Karpas-299 and Sup-M2) cells and ALK-negative lymphoma HuT-102 and leukemia Toledo cells; EML4-ALK–positive (NCI-H2228 and H3122) and EML4-ALK–negative (NCI-H1650) NSCLC cells and neuroblastoma cell lines |
| Preparation method | Cell growth inhibition Living cells were measured with the CellTiter 96 nonradioactive cell proliferation assay (MTS assay) kit. In brief, the cells were seeded on 96-well plates and 48 to 72 hours after compound treatment, equal volume of reagents from the kit was added to the culture medium. After incubation for 1 to 4 hours, the plates were measured with a plate reader and the relative cell numbers were calculated on the basis of the standard curve. |
| Concentrations | 0~10 μ M |
| Incubation time | 48 to 72 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID mice bearing NCI-H2228, NCI-H3122, and NCI-1650 (A) or NB-1 and NB-1691 (B) subcutaneous tumor xenografts |
| Formulation | PEG-400, or dH2O |
| Dosages | 3, 10, or 30 mg/kg twice a day for 10 days |
| Administration | oral |
| Molecular Weight | 539.07 |
| Formula | C28H35ClN6O3 |
| CAS Number | 1022958-60-6 |
| Solubility (25°C) | DMF: 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
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