Western blot analysis of extracts from SK-MEL-28 cells, untreated (-) or treated with Dabrafenib (GSK2118436) (1 μM, 24h; +), using Phospho-MEK1/2 (Ser217/221) (41G9) Rabbit mAb #9154 (upper), MEK1/2 (D1A5) Rabbit mAb #8727 (middle), or β-Actin (D6A8) Rabbit mAb #8457 (lower).
Chemical structure of Dabrafenib (GSK2118436).
Dabrafenib (GSK2118436) is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 962 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Molecular Weight: 519.6 g/mol
Molecular Formula: C23H20F3N5O2S2
Solubility: Soluble in DMSO at 30 mg/ml or ethanol at 1 mg/ml with slight warming.
Dabrafenib (GSK2118436) is a selective and potent B-Raf inhibitor. The compound inhibits mutant B-RafV600E and B-RafV600K with IC50 values of 0.6 nM and 0.5 nM, respectively, and is less effective at inhibiting wild-type B-Raf and C-Raf (IC50 = 3.2 nM and 5.0 nM, respectively) (1). Dabrafenib (GSK2118436) has also been shown to inhibit cell proliferation and ERK signaling in melanoma cell lines carrying the B-RafV600R and B-RafV600D mutations as compared to wild-type B-Raf (2). The specificity of this compound makes it a useful reagent when studying metastatic melanoma with B-Raf mutations (3).
This product has applications to SARS-CoV-2 research into the mechanisms of the Novel Coronavirus, which has caused the COVID-19 pandemic.
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