PD198306 , 98% , 212631-61-3
Synonym(s):
MEK Inhibitor VIII - CAS 212631-61-3 - Calbiochem;N-Cyclopropylmethoxy-3,4,5-trifluoro-2-(4-iodo-2-methylphenylamino)benzamide
CAS NO.：212631-61-3
Empirical Formula: C18H16F3IN2O2
Molecular Weight: 476.23
MDL number: MFCD08690428
| Pack Size | Price | Stock | Quantity |
| 1mg | RMB1050.40 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 125-127 °C |
| Density | 1.686±0.06 g/cm3(Predicted) |
| storage temp. | Store at +4°C |
| solubility | Soluble in DMSO |
| form | solid |
| pka | -3.95±0.50(Predicted) |
| color | White |
Description and Uses
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, 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. 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 or chronic constriction injury.
PD 198306 is a cell-permeable and highly selective potent inhibitor of MEK 1/2.
