Products & ReviewLife Sciences
PLX4032
MEK/ERK pathway inhibitor; Inhibits B-RAF
PLX4032
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PLX4032 is an ATP-competitive inhibitor of the serine/threonine kinase B-RAF proto-oncogene, with IC₅₀ values of 31 and 100 nM for the wild-type and V600E mutant forms respectively (Khazak et al.; Sala et al.).
CANCER RESEARCH
- Inhibits proliferation in colon, melanoma, and thyroid carcinoma cancer cell lines expressing B-RAF V600E, alone or in synergy with taxol, vinblastine, and oxaliplatin compounds (Khazak et al.).
- Suppresses MEK and ERK phosphorylation downstream of B-RAF in melanoma cells with mutations at the V600 position, correlated with antiproliferative effects (Joseph et al.; Yang et al.).
- Inhibits tumor growth in B-RAF V600E melanoma tumor xenograft models (Yang et al.).
