PLX4032, 50 mg

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

The compound is stable at -20°C as supplied and should be protected from prolonged exposure to light. Solubility in DMSO is reported at ≤ 2 mM, while solubility in aqueous media is low. For cell culture applications, stock solutions should be diluted into culture medium immediately before use, and final DMSO concentration should be kept below 0.1% to avoid potential cell toxicity. Stock solutions are recommended for storage in DMSO at -20°C, aliquoted into working volumes to limit repeated freeze-thaw cycles, with stability confirmed before each application.

Published cancer research applications include inhibition of proliferation in colon, melanoma, and thyroid carcinoma cell lines expressing B-RAF V600E, alone or in synergy with Paclitaxel, Vinblastine, and Oxaliplatin. The compound suppresses MEK and ERK phosphorylation downstream of B-RAF in melanoma cells carrying V600 mutations, an effect correlated with antiproliferative activity. It has also been shown to inhibit tumor growth in B-RAF V600E melanoma tumor xenograft models.