Background
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.
Molecular Formula
C23H20F3N5O2S2
Molecular Weight
519.6 g/mol
Purity
>98%
CAS
1195765-45-7
Solubility
Soluble in DMSO at 30 mg/ml or ethanol at 1 mg/ml with slight warming.
Storage
Directions for Use
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.
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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