CEP-28122
Modify Date: 2024-01-03 12:04:21
CEP-28122 structure
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Common Name | CEP-28122 | ||
|---|---|---|---|---|
| CAS Number | 1022958-60-6 | Molecular Weight | 539.069 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 786.9±70.0 °C at 760 mmHg | |
| Molecular Formula | C28H35ClN6O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 429.7±35.7 °C | |
Use of CEP-28122CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.IC50 value: 1.9 ± 0.5 nMTarget: ALKin vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small celllung cancer (NSCLC), and neuroblastoma cells. [1]in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1] |
| Name | cep-28122 |
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| Synonym | More Synonyms |
| Description | CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.IC50 value: 1.9 ± 0.5 nMTarget: ALKin vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small celllung cancer (NSCLC), and neuroblastoma cells. [1]in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1] |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 786.9±70.0 °C at 760 mmHg |
| Molecular Formula | C28H35ClN6O3 |
| Molecular Weight | 539.069 |
| Flash Point | 429.7±35.7 °C |
| Exact Mass | 538.245911 |
| PSA | 114.63000 |
| LogP | 1.47 |
| Vapour Pressure | 0.0±2.7 mmHg at 25°C |
| Index of Refraction | 1.665 |
| Storage condition | 2-8℃ |
| Bicyclo[2.2.1]hept-5-ene-2-carboxamide, 3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-, (1S,2S,3R,4R)- |
| (1S,2S,3R,4R)-3-[(5-Chloro-2-{[(7S)-1-methoxy-7-(4-morpholinyl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]amino}-4-pyrimidinyl)amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide |
| CEP 28122 |