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Trametinib | MEK inhibitor

Trametinib (871700-17-3) is a highly potent (IC50 uMEK1 = 0.7 nM, pp-MEK1 = 14.9 nM)1 and selective MEK inhibitor displaying selective inhibition of proliferation in various BRAF mutant cancer cell lines (IC50 ACHN = 9.8 nM; IC50 HT-29 = 0.57 nM)2. It is approved for use against unresectable or metastatic BRAF-mutant melanoma alone or in combination with Dabrafenib.  Trametinib can limit outgrowth of tumors without directly inhibiting tumor cell proliferation via abrogation of cytokine-driven expansion of monocytic myeloid-derived suppressor cells (mMDSC) through a mechanism involving CD8+ T cells.3,4 Trametinib also displays potent anti-arthritic effects.5


1) Gilmartin et al. (2011), GSK1120212 (JTP-74057) is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition; Clin. Cancer Res. 17 989
2) Abe et al. (2011), Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO solvate); ACS Med. Chem. Lett. 2 320
3) Allegrezza et al. (2016), Trametinib Drives T-cell-Dependent Control of KRAS Tumors by Inhibiting Pathological Myelopoiesis; Cancer Res. 76 6253
4) Vella et al. (2014), MEK inhibition, alone or in combination with BRAF inhibition, affects multiple functions of isolated normal human lymphocytes and dendritic cells; Cancer Immunol. Res. 2 351
5) Yamaguchi et al. (2012), Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with leflunomide; Inflamm. Res. 61 445

Focus Biomolecules cell signaling reagent supplier, chemical structure of Trametinib | MEK inhibitor | CAS 871700-17-3

Catalog#  10-4759-0010

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Catalog Number:
MEK inhibitor
Chemical Name:
Alternate Names:
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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