Trametinib

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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)
Datasheet
Citations
Reviews
Literature (4)
Pathways (1)

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.

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.

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

Reviews for Trametinib

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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.


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Pathways for Trametinib

MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.