| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 6.4 mg/mL (10.08 mM), Sonication is recommended.
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| Keywords | CEP28122 mesylate salt (1022958606 free base) | CEP-28122 Mesylate | CEP28122 Mesylate | CEP 28122 mesylate salt (1022958 60 6 free base) | CEP 28122 Mesylate | ALK | 1022958-60-6 free base | 1022958-60-6 |
| Inhibitors Related | Entrectinib | Alectinib hydrochloride | DMH-1 | SB-431542 | ALK-IN-1 | RepSox | Crizotinib | Vactosertib | Ceritinib | LDN-193189 2HCl | Brigatinib | A 83-01 |
| 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 | Angiogenesis related Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
