CEP-28122 mesylate salt

• CAT Number: I005871
• Molecular Formula: C29H39ClN6O6S
• Molecular Weight: 635.17
• Purity: ≥95%
• Target: ALK
• Solubility: DMSO: ≥ 6.4 mg/mL, DMSO ＜ 9.2 mg/mL
• Storage: Store at -20°C
• IC50: 1.9 ± 0.5 nM

CEP-28122 mesylate salt 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 nM 


Target: ALK 


in 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 cell
lung cancer (NSCLC), and neuroblastoma cells. 


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. 
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Reference

[1]. Cheng M, et al. CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2012 Mar;11(3):670-679.