Interested in promotions? | Click here >>
62206
Trametinib
Activators & Inhibitors
Chemical Modulators

Trametinib #62206

Reviews ()
Citations (0)
Trametinib: Image 1
Western blot analysis of extracts from HeLa cells, untreated (-) or treated with TPA #4174 (200 nM, 20 min; +) with or without pretreating the cells with Trametinib for 1 hour at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370 (upper), p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695 (middle), and β-Actin (D6A8) Rabbit mAb #8457 (lower).
Trametinib: Image 2
Chemical structure of Trametinib.

Product Usage Information

Trametinib is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 10 mg of powder in 1.08 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

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.

Product Description

Molecular Weight 615.4 g/mol
Purity >98%
Molecular Formula C26H23FIN5O4
CAS 871700-17-3
Solubility Soluble in DMSO at 20 mg/ml with slight warming.

Background

Trametinib, also known as GSK1120212, is a potent and selective inhibitor of MEK with an IC50 of 0.7 nM for u-MEK1 and 14.9 nM for pp-MEK1 (1). When compared to several tyrosine kinase inhibitors (TKIs) and MEK inhibitors (MEKIs) in endothelial cells, Trametinib displays the highest level of antiangiogenic activity and is the most effective ERK1/2 inhibitor (IC50 = 1.3 nM) (2). Trametinib has also been shown to be the most effective at reducing proliferation in low-grade serous ovarian cancers (LGSCs) when compared to other MEKIs (3).
  1. Gilmartin, A.G. et al. (2011) Clin Cancer Res 17, 989-1000.
  2. Bridgeman, V.L. et al. (2016) Mol Cancer Ther 15, 172-83.
  3. Fernández, M.L. et al. (2016) Am J Cancer Res 6, 2235-51.

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.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.
To Purchase # 62206
Cat. # Size Qty. Price
62206S
10 mg $ 96