Definition

An orally available inhibitor of class I, II, and III B-Raf (BRAF) protein kinases, with potential antineoplastic activity. Upon administration, pan-Raf inhibitor KIN-2787 binds to and inhibits Class I, Class II, or Class III B-Raf mutations. This prevents B-Raf-mediated signal transduction pathways, which may lead to an inhibition of tumor growth in B-Raf mutant cells. B-Raf protein kinases play a key role in the RAF/MEK/ERK signaling pathway, which is often deregulated and mutated in human cancers, and plays a key role in tumor cell proliferation and survival.