PD 198306

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2605/10
PD 198306 | CAS No. 212631-61-3 | MEK Inhibitors
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Description: Selective inhibitor of MEK1/2

Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide

Purity: ≥98%

Product Details
Citations (2)
Reviews (1)

Biological Activity

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.

Technical Data

M.Wt:
476.23
Formula:
C18H16F3IN2O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
212631-61-3

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.

Background References

  1. Identification of MEK1 as a novel target for the treatment of neuropathic pain.
    Ciruela et al.
    Br.J.Pharmacol., 2003;138:751
  2. 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.
    Pelletier et al.
    Arthrit.Rheumat., 2003;48:1582

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Citations for PD 198306

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2 Citations: Showing 1 - 2

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In vitro culture
By Anonymous on 08/05/2018
Application: Species: Human

Used in vitro as ERK inhibitor in SH-SY5Y at 10 uM. Good performance.


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