CEP-28122 mesylate salt (1022958-60-6 free base) 是一种高选择性的口服活性 ALK 抑制剂（在基于酶的 TRF 测定中，IC50：1.9 nM）。

CEP-28122 mesylate salt is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).

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).

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.

T10759

C29H39ClN6O6S

635.17

CEP-28122 mesylate salt

DMSO:6.4 mg/mL (10.08 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years