NCIt 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.;