A potent inhibitor of MEK1/2
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PD 198306

Item No. 23966

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide
CAS Number
212631-61-3
Molecular Formula
C18H16F3IN2O2
Formula Weight
476.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 100 mM
SMILES
CC1=CC(I)=CC=C1NC2=C(F)C(F)=C(F)C=C2C(NOCC3CC3)=O
InChi Code
InChI=1S/C18H16F3IN2O2/c1-9-6-11(22)4-5-14(9)23-17-12(7-13(19)15(20)16(17)21)18(25)24-26-8-10-2-3-10/h4-7,10,23H,2-3,8H2,1H3,(H,24,25)
InChi Key
UHAXDAKQGVISBZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $74

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    5 mg

    $255

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    10 mg

    $399

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    Product Description

    PD 198306 is an orally bioavailable and potent inhibitor of MAPK kinase 1/2 (MEK1/2; IC50 = 8 nM).1 It is selective for MEK1/2 over ERK, c-Src, PI3Kγ, and cyclin-dependent kinases (IC50s = >1 μM). PD 198306 (3-100 μM) reduces ERK1/2 phosphorylation and inhibits growth of HL-60 cells in vitro.2 In vivo, PD 198306 (10-30 mg/kg) reduces ERK1/2 phosphorylation and matrix metalloproteinase-1 (MMP-1) expression in a dose-dependent manner in a rabbit model of osteoarthritis.1 It also reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of neuropathic pain induced by streptozotocin (Item No. 13104) or chronic constriction injury.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pelletier, J.P., Fernandes, J.C., Brunet, J., et al. In vivo selective inhibition of mitogen-activated protein kinase kinase ½ in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthritis Rheum. 48(6), 1582-1593 (2003).

    2. Ripple, M.O., Kim, N., and Springett, R. Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) ½ inhibitors regulates proliferation. The Journal of Biological Chemisty 288(5), 2933-2940 (2013).

    3. Ciruela, A., Dixon, A.K., Bramwell, S., et al. Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br. J. Pharmacol. 138(5), 751-756 (2003).