PLX4032 is an ATP-competitive inhibitor of the serine/threonine kinase B-RAF proto-oncogene, with IC50 values of 31 and 100 nM for the wild-type and V600E mutant forms respectively (Khazak et al.; Sala et al.)
Inhibits proliferation in colon, melanoma, and thyroid carcinoma cancer cell lines expressing B-RAF V600E, alone or in synergy with taxol, vinblastine, and oxaliplatin compounds (Khazak et al.)
Suppresses MEK and ERK phosphorylation downstream of B-RAF in melanoma cells with mutations at the V600 position, correlated with antiproliferative effects (Joseph et al.; Yang et al.)
Inhibits tumor growth in B-RAF V600E melanoma tumor xenograft models (Yang et al.)
