Trametinib
Tocris Bioscience, part of Bio-Techne | Catalog # 7709
Potent and selective MEK inhibitor; orally bioavailable
Key Product Details
Description
Potent and selective MEK inhibitor; orally bioavailable
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
Molecular Weight
615.40
Formula
C26H23FIN5O4
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 615.40
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for Trametinib
For research use only
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