PD 198306

Product Description

PD 198306 is a 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.

Solubility

Preparing Stock Solutions for PD 198306

The following data is based on the product molecular weight 476.23

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.

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

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.10 mL	10.50 mL	21.00 mL
5 mM	0.42 mL	2.10 mL	4.20 mL
10 mM	0.21 mL	1.05 mL	2.10 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Pelletier 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.
• Ciruela Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br.J.Pharmacol. 2003 PMID: 12642375