Biological Activity
Potent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30 - 100 nM. Highly selective for MEK; IC50 values are > 1, > 4, > 4 and > 10 μM for ERK, c-Src, cdks and PI 3-kinase γ respectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.
Technical Data
| M. Wt | 476.23 |
| Formula | C18H16F3IN2O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 212631-61-3 |
| PubChem ID | 9956637 |
| InChI Key | UHAXDAKQGVISBZ-UHFFFAOYSA-N |
| Smiles | CC1=C(NC2=C(C=C(F)C(F)=C2F)C(=O)NOCC2CC2)C=CC(I)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.62 | 100 | |
| ethanol | 47.62 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 476.23. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.1 mL | 10.5 mL | 21 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.2 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.1 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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References
References are publications that support the products' biological activity.
Ciruela et al (2003) Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br.J.Pharmacol. 138 751 PMID: 12642375
Pelletier et al (2003) In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthrit.Rheumat. 48 1582 PMID:
Keywords: PD 198306, supplier, Selective, inhibitors, inhibits, MEK1/2, Mitogen-Activated, Protein, Kinase, kinases, PD198306, MEK, MEK, Tocris Bioscience
