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 displays 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.
Molecular Weight:
518.61
CAS Number:
[856692-39-2]
Formula:
C31H30N6O2
Target:
Others|||Tie-2|||VEGFR|||IGF-1R|||ALK
T68538
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