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Stemcell 73502 Trametinib
Product Overview
Trametinib is an allosteric, reversible, non-ATP competitive inhibitor of mitogen-activated protein kinase kinases (MEK) isoforms MEK1 and MEK2 with IC₅₀ values of 0.7 and 0.9 nM, respectively (Gilmartin et al.; Yoshida et al.). It is specific for MEK versus > 100 other kinases (Yamaguchi et al.).
CANCER RESEARCH
· Inhibits growth in multiple cell lines, especially those with B-RAF V600, other RAF/RAS-activating, or β-catenin mutations (Gilmartin et al.; Jing et al.; Yamaguchi et al.; Uitdehaag et al.).
· Delays tumor growth and causes tumor regression in mouse xenograft models with various cancer cell types containing B-RAF or K-RAS mutations (Gilmartin et al.; Yamaguchi et al.).
CAS Number:871700-17-3
Alternative Names:GSK 1120212, G 02442104, JTP-74057, Mekinist
Chemical Formula:C₂₆H₂₃FIN₅O₄
Molecular Weight:615.4 g/mol
Purity:≥ 95%
Pathway:MEK/ERK
Target:MEK1; MEK2
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