PLX4032, 10 mg

An ATP-competitive inhibitor of the serine/threonine kinase B-RAF proto-oncogene, this small molecule has IC₅₀ values of 31 and 100 nM for the wild type and V600E mutant forms, respectively. Also known by alternative names RG-7204, Ro 51-85426, Vemurafenib, and Zelboraf™, it has a CAS number of 918504-65-1, a molecular formula of C₂₃H₁₈ClF₂N₃O₃S, and a molecular weight of 489.9 g/mol. The product is supplied by STEMCELL Technologies as a crystalline solid with a purity of ≥ 98%.

In cancer research, this compound inhibits proliferation in colon, melanoma, and thyroid carcinoma cancer cell lines expressing B-RAF V600E, alone or in synergy with Paclitaxil, Vinblastine, and Oxaliplatin. It suppresses MEK and ERK phosphorylation downstream of B-RAF in melanoma cells with mutations at the V600 position, correlated with antiproliferative effects, and inhibits tumor growth in B-RAF V600E melanoma tumor xenograft models.

Stable at -20°C as supplied and should be protected from prolonged exposure to light, the compound has low solubility in aqueous media but can be dissolved in DMSO at concentrations of ≤ 2 mM. For use as a cell culture supplement, stock solutions should be diluted into culture medium immediately before use, and final DMSO concentration above 0.1% should be avoided due to potential cell toxicity.