Trametinib

Key Product Details

Product Description

Trametinib is a potent and selective MEK1 and MEK2 inhibitor (IC₅₀ = 0.92 and 1.8 nM, respectively, in cell-free assays). In vitro, it inhibits the growth of human colorectal cancer cell lines expressing either B-RAF or K-RAF (IC₅₀ values range from 0.48 to 36 nM). In vivo, it suppresses tumor growth of HT-29 and COLO205 xenografts in nude mice. Trametinib induces apoptosis. This compound is orally bioavailable.

Product Specifications for Trametinib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Trametinib

The following data is based on the product molecular weight 615.40.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.62 mL	8.12 mL	16.25 mL
5 mM	0.32 mL	1.62 mL	3.25 mL
10 mM	0.16 mL	0.81 mL	1.62 mL
50 mM	0.03 mL	0.16 mL	0.32 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 15 publications citing the usage of this product.

• Kobelt The newly identified MEK1 tyrosine phosphorylation target MACC1 is druggable by approved MEK1 inhibitors to restrict colorectal cancer metastasis. Oncogene 2021 PMID: 34247190
• Zhao Diverse alterations associated with resistance to KRAS(G12C) inhibition. Nature 2021 PMID: 34759319
• Yamaguchi 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 PMID: 21523318

Product Documents for Trametinib