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Submit ReviewTrametinib
Description: Potent and selective MEK inhibitor; orally bioavailable
Chemical Name: 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
Purity: ≥98% (HPLC)
Biological Activity for Trametinib
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.
Compound Libraries for Trametinib
Trametinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for Trametinib
| M. Wt | 615.4 |
| Formula | C26H23FIN5O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 871700-17-3 |
| PubChem ID | 11707110 |
| InChI Key | LIRYPHYGHXZJBZ-UHFFFAOYSA-N |
| Smiles | O=C(NC1=CC=CC(=C1)N2C(=O)N(C(=O)C3=C(NC4=CC=C(I)C=C4F)N(C(=O)C(=C32)C)C)C5CC5)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Trametinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 61.54 | 100 |
Preparing Stock Solutions for Trametinib
The following data is based on the product molecular weight 615.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Product Datasheets for Trametinib
References for Trametinib
References are publications that support the biological activity of the product.
Yamaguchi et al (2011) Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int.J.Oncol. 39 23 PMID: 21523318
Kobelt et al (2021) The newly identified MEK1 tyrosine phosphorylation target MACC1 is druggable by approved MEK1 inhibitors to restrict colorectal cancer metastasis. Oncogene 40 5286 PMID: 34247190
Zhao et al (2021) Diverse alterations associated with resistance to KRAS(G12C) inhibition. Nature 599 679 PMID: 34759319
If you know of a relevant reference for Trametinib, please let us know.
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Keywords: Trametinib, Trametinib supplier, Potent, inhibitors, inhibits, MEK1, MEK2, MEK, Mitogen-Activated, Protein, Kinase, Kinases, orally, bioavailable, 7709, Tocris Bioscience
Citations for Trametinib
Citations are publications that use Tocris products.
Currently there are no citations for Trametinib. Do you know of a great paper that uses Trametinib from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for Trametinib
