Background
Vemurafenib, also known as PLX4032, is an inhibitor of mutated BRAF (V600E) (1,2). The BRAF kinase is responsible for the activation of MEK and in turn, activating ERK and other downstream transcription factors involved in cell differentiation, proliferation, growth and apoptosis (1). The V600E mutation elevates the catalytic activity of BRAF which in turn renders it insensitive to negative feedback, thus causing hyperactivation of ERK signaling (2). Ultimately, the inhibition of mutated BRAF will cause a cascade of inhibitory actions against downstream targets, such as ERK and MEK1/2 (1,2).
Molecular Formula
C23H18CIF2N3O3S
Molecular Weight
489.92 g/mol
Purity
>99%
CAS
918504-65-1
Solubility
Soluble in DMSO at 100mg/ml.
Storage
Directions for Use
Vemurafenib is supplied as a lyophilized powder. For a 50 mM stock, reconstitute the 5 mg of powder in 204.12 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used between 0.5-50 μM for 24 hrs.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
Limited Uses
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