IC50: 8 nM for MEK PD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor. MEK is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). In vitro: PD 198306 inhibits the isolated MEK at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at 30–100 nM, depending on the species. PD 198306 is highly selective for MEK and has a IC50 of >4 uM for c-Src, >1 uM for ERK, >4 uM for cyclin-dependent kinases and >10 uM for phosphatidylinositol 3-kinase . In vivo: Rabbits treated with PD 198306 showd a significant dose-dependent reduction in the level of phospho-ERK-1/2 and a lower level of MMP-1. PD 198306 can partially decrease the development of some of the structural changes in experimental rabbit model of osteoarthritis . PD 198306 dose-dependently blocked static allodynia in both the streptozocin and the chronic constriction injury models of neuropathic pain. These antihyperalgesic effects correlated with a reduction in the elevated levels of active ERK1 and 2 in lumbar spinal cord . Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 212631-61-3

Molecular Weight: 476.23

Formula: C18H16F3IN2O2

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

Smiles: CC1=CC(I)=CC=C1NC1=C(C=C(F)C(F)=C1F)C(=O)NOCC1CC1

InChiKey: UHAXDAKQGVISBZ-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.