PLX4720
Mutant B-Raf inhibitor / 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
Biochemicals & reagents
918505-84-7
1 Tsai et al. (2008), Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity; Proc. Natl. Acad. Sci. USA, 105 3041 2 Nehs et al. (2012), Late intervention with anti-BRAF(V600E) therapy induces tumor regression in an orthotopic mouse model of human anaplastic thyroid cancer; Endocrinology, 153 985 3 Yeom et al. (2021), Increase in the sensitivity to PLX4720 through inhibition of transcription factor EB-dependent autophagy in BRAF inhibitor-resistant cells; Toxicol. Res., 38 35 4 Jimenez-Morah et al. (2021), V600EBRAF Inhibition Induces Cytoprotective Autophagy through AMPK in Thyroid Cancer Cells; Int. J. Mol. Sci. 22 6033
-20°C
TARGET: Kinase; Cytochrome/MDR -- PATHWAY: Autophagy; Cytokine; MAPK -- DISEASE AREA: Cancer