PD 198306

PD 198306 is an orally bioavailable and potent inhibitor of MAPK kinase 1/2 (MEK1/2, IC50 = 8 nM). It is selective for MEK1/2 over ERK, c-Src, PI3Kgamma, 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. 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. It also reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of neuropathic pain induced by streptozotocin (Cay-13104) or chronic constriction injury.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: DMSO: 100 mM, Ethanol: 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.