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Trametinib (GSK1120212)

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Catalog No.
MEK1 and MEK2 inhibitor, potent and selective
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SizePriceStock Qty
10mM (in 1mL DMSO)
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Evaluation Sample
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Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.


Akintunde Akinleye, Muhammad Furqan, Nikhil Mukhi, Pavan Ravella and Delong Liu. MEK and the inhibitors: from bench to bedside. Journal of Hematology & Oncology 2013, 6:27

Motoki Watanabe, Yoshihiro Sowa, Mayumi Yogosawa and Toshiyuki Sakai. Novel MEK inhibitor trametinib and other retinoblastoma gene (RB)-reactivating agents enhance efficacy of 5-fluorouracil on human colon cancer cells. Cancer Sci 2013; 104(6): 687-693

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.871700-17-3
SynonymsTrametinib, GSK-1120212, GSK1120212, Mekinist, JTP74057, JTP-74057
Solubility≥15.38mg/mL in DMSO
Chemical NameN-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide
SDFDownload SDF
Canonical SMILESCC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.


Cell experiment: [1]

Cell lines

HT-29 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

100 nM, 72 hours


Trametinib showed a subnanomolar IC50 value for 72 h in a Cell Counting Kit-8 assay of human colon cancer HT-29 cells. The treatment with trametinib for 24 h dose-dependently increased the G1 phase with a decrease in the S phase, and 72 h treatment induced apoptosis in a dose-dependent manner together with G1 arrest.

Animal experiment: [2]

Animal models

Male ICR mice

Dosage form

Oral administration, 3 mg/kg, daily


GSK1120212 was effective at blocking phosphorylation of ERK over 24 h and 7 d. To test whether the inhibitor blocked adaptive growth, mice were treated with GSK1120212 and/or the trypsin inhibitor camostat mesylate S (TI) for 7 d. TI-induced pancreatic growth was blocked by GSK1120212 as measured by pancreatic mass, protein, DNA, and RNA content. These results show that GSK1120212 like PD0325901 blocks pancreatic adaptive growth induced by TI.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Watanabe M, Sowa Y, Yogosawa M, et al. Novel MEK inhibitor trametinib and other retinoblastoma gene (RB)-reactivating agents enhance efficacy of 5‐fluorouracil on human colon cancer cells. Cancer science, 2013, 104(6): 687-693.

[2] Holtz B J, Lodewyk K B, Sebolt-Leopold J S, et al. ERK Activation is Required for CCK-mediated Pancreatic Adaptive Growth in Mice. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2014: ajpgi. 00163.2014.

Biological Activity

Description Trametinib (GSK1120212) is a highly specific and potent inhibitor of MEK1/2 with IC50 of 0.92 nM/1.8 nM.
Targets MEK1 MEK2        
IC50 0.92 nM 1.8 nM        

Quality Control

Chemical structure

Trametinib (GSK1120212)

Related Biological Data

GSK1120212 causes sustained inhibition of ERK1/2 phosphorylation, and differential effects on MEK phosphorylation. SK-MEL-28 and A-375P(F11) (BRAF-mutant) cell lines were treated with 250 nmol/L GSK1120212 (Trametinib) and harvested at the indicated time points.

Related Biological Data

Trametinib (GSK1120212)

Related Biological Data

Trametinib (GSK1120212)

Related Biological Data

Trametinib (GSK1120212)

Related Biological Data

Trametinib (GSK1120212)

Research Update

1. Comprehensive predictive biomarker analysis for MEK inhibitor GSK1120212. Mol Cancer Ther. 2012 Mar;11(3):720-9. doi: 10.1158/1535-7163.MCT-11-0505. Epub 2011 Dec 14.
GSK1120212, an inhibitor of MEK1 and MEK2, is sensitive to various cell lines including RAF/RAS mutant solid tumor cell lines, breast cancer cell lines, acute myeloid leukemia cell lines and chronic myeloid leukemia cell lines and is less sensitive to cell lines with an expression pattern suggestive of epithelial-to-mesenchymal transition, where expression of gene DUSP6 was associated with GSK1120212 sensitivity.
3. Trametinib (GSK1120212) in the treatment of melanoma. Expert Opin Pharmacother. 2013 Apr;14(5):619-27. doi: 10.1517/14656566.2013.770475. Epub 2013 Feb 23.
Somatic mutations involved in MAPK pathway, including NRAS, BRAF, GNAQ and GNA11, are associated with melanoma. Targeting MEK has the potential to be incorporated into the treatment of melanoma patients with those mutations.
4. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011 Jul;39(1):23-31. doi: 10.3892/ijo.2011.1015. Epub 2011 Apr 26.
GSK1120212 is an inhibitor of MEK1/2 that exhibits antitumor activity against colorectal cancer cells through growth inhibition and induced apoptosis. Addition of an Akt inhibitor or a few standard-of-care agents could enhance the antitumor activity of GSK1120212.