| Name | CEP-28122 mesylate salt (1022958-60-6 free base) |
| Description | CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay). |
| In vitro | CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 (IC50: 46 nM). CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), neuroblastoma cells, and non-small cell lung cancer (NSCLC). |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 6.4 mg/mL (10.08 mM)
|
| Keywords | CEP 28122 mesylate salt (1022958 60 6 free base) | 1022958-60-6 | CEP 28122 Mesylate | CEP28122 mesylate salt (1022958606 free base) | CEP-28122 Mesylate | 1022958-60-6 free base | CEP28122 Mesylate |
| Inhibitors Related | Alectinib hydrochloride | Lorlatinib | SB-431542 | DMH-1 | RepSox | Crizotinib | Vactosertib | Ceritinib | LDN-193189 2HCl | Brigatinib | A 83-01 | ALK-IN-1 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Hematonosis Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
