CGP57380

CGP57380 is a selective, small molecule inhibitor of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1), with reported inhibitory activity against MNK2 as well. It is a pyrazolopyrimidine derivative with a 4-fluorophenyl group. CGP57380 inhibits MNK1-mediated phosphorylation of eIF4E, which downregulates translation of mRNAs involved in oncogenesis and cell survival, such as Mcl-1, Bcl-2, c-Myc, and cyclin D1. In preclinical studies, it has demonstrated ability to induce apoptosis and suppress tumor growth in models of T-cell acute lymphoblastic leukemia, non-small cell lung cancer, and other cancer cell lines, particularly when used in combination with other agents targeting the mTOR pathway[1][5].

Other names

N3-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine522629-08-9CHEMBL1240885CHEMBL-1240885CHEMBL 1240885CHEBI:92749NSC741567NSC-741567NSC 741567