PLX4032 (Vemurafenib) is an 7-azaindole-based, orally-available, inhibitor of the B-Raf V600E mutation with
an IC50 of 30 nM.  In preclinical tumor models, PLX4032 induces antiproliferative effects in both
mealonama and thyroid cell lines, with a simultaneous dose-dependent block of MEK1/2 phosphorylation.
 Apoptosis is also observed in melanoma cell lines upon treatment with PLX4032. Important to note is that
proliferation was inhibited in tumor cell lines expressing B-Raf V600E only, and not B-Raf WT or other B-Raf
PLX4032 has marginal effect on cell-cycle arrest, apoptotic cell changes, or alteration of phosphorylated
signaling molecules in lymphocytes. T-cell function was preserved up to 10 uM of PLX4032, while cytotoxic
activty was maintained up to high concentrations of 50 uM.  Such observations suggest that PLX4032 can
be used in combination with immunotherapy strategies.