Revision 1

#91942

Store at -20C

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Orders:

877-616-CELL (2355)

[email protected]

Support:

877-678-TECH (8324)

3 Trask Lane | Danvers | Massachusetts | 01923 | USA

For Research Use Only. Not for Use in Diagnostic Procedures.

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

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.

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.

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 G: Goat All: All Species Expected

Trademarks and Patents

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.

All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

Orders: 877-616-CELL (2355) [email protected] Support: 877-678-TECH (8324) [email protected] Web: cellsignal.com
For Research Use Only. Not for Use in Diagnostic Procedures.

Revision 1

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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).

undefined Image 1: Dabrafenib (GSK2118436)

Chemical structure of Dabrafenib (GSK2118436).

undefined Image 2: Dabrafenib (GSK2118436)
Orders: 877-616-CELL (2355) [email protected] Support: 877-678-TECH (8324) [email protected] Web: cellsignal.com
For Research Use Only. Not for Use in Diagnostic Procedures.