RAF inhibitor DCC-3084

An orally bioavailable central nervous system (CNS)-penetrant switch control inhibitor of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon oral administration, RAF inhibitor DCC-3084 targets and binds to BRAF and CRAF kinases, including BRAF monomeric class I mutation, dimeric class II (Ras-independent) and class III (Ras-dependent) mutations, BRAF fusions and BRAF/CRAF heterodimers, specifically at the switch pocket regions, thereby binding both monomers of the RAF dimers and preventing paradoxical activation that results from unbound monomers. This prevents the activation of Raf-mediated signal transduction pathways, which may inhibit tumor cell growth. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. They play key roles in tumor cell proliferation and survival.