PLX4032 (Vemurafenib) is an 7-azaindole-based, orally-available, inhibitor of the B-Raf V600E mutation with an IC50 of 30 nM. [1] 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. [1] 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 mutations. [2]

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. [3] Such observations suggest that PLX4032 can be used in combination with immunotherapy strategies.

PLX4032 (Vemurafenib) is an 7-azaindole-based, orally-available, inhibitor of the B-Raf V600E mutation with an IC50 of 30 nM. [1] 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. [1] 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 mutations. [2]

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. [3] Such observations suggest that PLX4032 can be used in combination with immunotherapy strategies.