PLX4720

Potent and selective inhibitor of B-Raf, V600E mutant, IC50=13 nM (Wild type IC50=160 nM) .1 It induces cell cycle arrest and apoptosis in B-RafV600E-positive cells and suppresses growth of B-RafV600E-positive xenografts.1 It induces tumor regression and reverses cachexia in a mouse model of human thyroid cancer harboring the B-RafV600E mutation.2 Early stage autophagy inhibitors and ER stress inhibition with 4-phenylbutyric acid increases the sensitivity of resistant cells to PLX4720.3 PLX4720 induces cytoprotective autophagy in thyroid cancer cells via AMPK-ULK1 pathway.4