Product Name:

Trametinib(GSK-1120212, JTP-74057)

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CAT#: A-1258    

Chemical Structure

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Biological Activity

Trametinib, also known as GSK1120212, is an orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. GSK-1120212 is a MEK inhibitor in clinical trials
Technical Data

Formula:C26H23FIN5O4
M.W.: 615.39
CAS#: 871700-17-3
Solubility: Soluble in DMSO
Purity: > 99% by HPLC
Storage: 2oC to 8 oC, or -20oC for long-term storage
Synonyms: N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]acetamide
GSK-1120212 MSDS GSK-1120212 CoA
Reference

Safety and efficacy results from the first-in-human study of the oral MEK 1/2 inhibitor GSK1120212.
J. R. Infante, L. A. Fecher, S. Nallapareddy, M. S. Gordon, K. T. Flaherty, D. S. Cox, D. J. DeMarini, S. R. Morris, H. A. Burris and W. A. Messersmith

B-RAF inhibitors: an evolving role in the therapy of malignant melanoma
C Shepherd, I Puzanov...- Current oncology reports, 2010 - Springer
... It is completing phase 1 studies, as well, and about to enter phase 2/3 trials as GSK2118436. Development appears to be proceeding rapidly and very effectively. Discussions are also underway in efforts to combine this BRAF inhibitor with a GSK MEK inhibitor (GSK 1120212). ...

Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo.
T Yamaguchi, R Kakefuda, N Tajima...-...journal of oncology, 2011 - ncbi.nlm.nih.gov
The MAPK pathway is one of the most important pathways for novel anticancer drug development. We performed high-throughput screening for compounds that induce expression of p15INK4b, and identified JTP-74057 (GSK1120212), which is being evaluated in ...