CB-1158-analog

Биологическая активность

CB-1158-analog, also known as Numidargistat-analog and INCB01158-analog, is a мощный and orally active arginase ингибитор с IC50=89 nM) . CB-1158 blocked myeloid клетка-mediated suppression of T клетка proliferation in vitro and reduced tumor growth in multiple mouse models of cancer, as a single agent and in combination with checkpoint blockade, adoptive T клетка therapy, adoptive NK клетка therapy, and the chemotherapy agent gemcitabine. CB-1158 increased tumor-infiltrating CD8+ T cells and NK cells, inflammatory cytokines, and expression of interferon-inducible genes. CB-1158 may be potentially useful in renal клетка cancer, breast cancer, non-small клетка lung cancer, acute myeloid leukemia, and other tumor types where arginase-secreting MDSCs are known to play an immunosuppressive role. (see ADDITIONAL INFORMATION in this web page for CB-1158 structure confusion).