CEP-28122
CEP-28122, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 has good pharmacodynamic and pharmacokinetic activity. CEP-28122 can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells.
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- CAS No.: 1022958-60-6
- Formule: C28H35ClN6O3
- Masse moléculaire:539.07
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
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| KARPAS-299 | IC50 |
20 nM
Compound: 25b, diasteromer 2
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Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma
Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma
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[PMID: 22564207] |
CEP-28122 (3-3000 nM; 48 hours) treatment leads to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture, associates with concentration-related caspase 3/7 activation[1]. CEP-28122 (30-1000 nM; 2 hours) treatment leads to substantial suppression of phosphorylation of putative downstream effectors of ALK in Sup-M2 cells, indicating that the downstream signaling pathways are mediated by individual ALK fusion protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Karpas-299, Sup-M2, Toledo and HuT-102 cells
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Concentration:10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:48 hours
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Result:Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.
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Cell Line:Sup-M2 cells
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Concentration:30 nM, 100 nM, 300 nM, 1000 nM
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Incubation Time:2 hours
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Result:Resulted in substantial suppression of phosphorylation of putative downstream effectors of ALK, including Stat-3, Akt, and ERK1/2 in Sup-M2 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and nu/nu mice bearing HCT116 aged 6-8 week old[1]
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Dosage:3 mg/kg, 10 mg/kg and 30 mg/kg
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Administration:oral gavage; twice a day; 12 days
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Result:Produced dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice. Had no antitumor activity in nu/nu mice bearing HCT116.
Chemical Information
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CAS No. 1022958-60-6
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Masse moléculaire 539.07
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Formule C28H35ClN6O3
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SMILES
O=C([C@H]1[C@](C2)([H])C=C[C@]2([H])[C@H]1NC3=NC(NC4=CC=C5C(CC[C@@H](N6CCOCC6)CC5)=C4OC)=NC=C3Cl)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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