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17531
Vemurafenib

Vemurafenib #17531

Western Blotting

Western blot analysis of extracts from SK-MEL-28 cells, untreated (-) or treated with Vemurafenib (24 hr) at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370, p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695, Phospho-MEK1/2 (Ser217/221) (41G9) Rabbit mAb #9154, and MEK1/2 (D1A5) Rabbit mAb #8727.

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Structure

Chemical structure of Vemurafenib.

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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.

Storage:

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Molecular Weight:

489.92 g/mol

Purity:

>99%

Molecular Formula:

C23H18CIF2N3O3S

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).

  1. Cantwell-Dorris, E.R. et al. (2011) Mol Cancer Ther 10, 385-94.
  2. Joseph, E.W. et al. (2010) Proc Natl Acad Sci U S A 107, 14903-8.
For Research Use Only. Not For Use In Diagnostic Procedures.

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