Definition

An orally bioavailable, small molecule inhibitor of mutant (V600E) v-raf murine sarcoma viral oncogene homolog B1 (BRAF) with potential antineoplastic activity. Upon oral administration, BRAF(V600E) kinase inhibitor ABM-1310 selectively binds to and inhibits the activity of BRAF(V600E) kinase, which may result in the inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. BRAF belongs to the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway. The valine to glutamic acid substitution at residue 600 accounts for about 90% of BRAF gene mutations. The oncogenic product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) mutation has been found to occur in about 8% of all tumors.