CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALKA–carrying T-cell lymphoma in vitro study. Presumably, this compound binds to the hinge region of the kinase in an ATP-competitive manner. CEP-14083 exhibits a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). Further, CEP-14083 is also able to inhibit the insulin receptor at a concentration within a nanomolar range. In a preclinical assay, CEP-14083 showed that, via NPM/ALK TK inhibition, it could control the expression of molecules that determine T-cell identity and signaling in lymphoma cells. CEP-14083 has shown preclinical activity in both cell lines and animal models harboring ALK alteration. References: Marzec M, Halasa K, Liu X, Wang HY, Cheng M, Baldwin D, Tobias JW, Schuster SJ, Woetmann A, Zhang Q, Turner SD, A~dum N, Wasik MA. Malignant transformation of CD4+ T lymphocytes mediated by oncogenic kinase NPM/ALK recapitulates IL-2-induced cell signaling and gene expression reprogramming. J Immunol. 2013 Dec 15;191(12):6200-7. doi: 10.4049/jimmunol.1300744. Epub 2013 Nov 11. PubMed PMID: 24218456; PubMed Central PMCID: PMC3889215.

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CAS：856692-39-2