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CEP-28122

CAS No. : 1022958-60-6

Biological Activity：CEP-28122 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. [1]
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. [1]

Research Area：Cancer

Targets：Anaplastic lymphoma kinase (ALK)

Related Small Molecules:ALK-IN-9;KRCA-0008;Alectinib-d8;MS4078;TL13-22;NVP-TAE 684;ALK5-IN-30;TL13-112;ALK-IN-22;Alectinib;ALK-IN-12;Entrectinib;ALK kinase inhibitor-1;WY-135;TL13-110;ALK inhibitor 1;Envonalkib;GSK1838705A;RIPK2-IN-1;CJ-2360;ALK-IN-1;ALK5-IN-29;X-376;ALK-IN-21;Repotrectinib;Lorlatinib;M4K2234;MS4077

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