Trametinib

Name: Trametinib
Brand: Tocris Bioscience
SKU: 7709

Tocris Bioscience, part of Bio-Techne | Catalog # 7709

Citations (12)

COA / SDS

Potent and selective MEK inhibitor; orally bioavailable

Key Product Details

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)
Molecular Weight:	615.4

View Full Technical Details for Trametinib

Technical Data
Citations

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 for Trametinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for Trametinib

References are publications that support the biological activity of the 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