Figure 2. Antiproliferative activity of 1t is associated with the presence of mutant BRAF.
(A) Antiproliferative effect of 1t following a 5-d exposure across a panel of human melanoma, colon and breast cancer cell lines, determined by SRB assay. (B) WM266.4 (V600DBRAF) and SW620 (G12VKRAS) cells were treated with 0.1 μM of 1t for 24 h and DNA synthesis determined using [3H]-thymidine. (C) Kinase activity of recombinant V600EBRAF (VE) and T529N,V600EBRAF (NVE) in the presence of 1t measured using DELFIA assay. (D) Inhibition of BRAF-mediated MEK/ERK activation in Ba/F3 cells expressing V600EBRAF or T529N,V600EBRAF following a 2 h exposure. DNA synthesis in Ba/F3 cells driven by V600EBRAF (VE) or T529N,V600EBRAF (NVE) following a 24 h exposure to 1t.