| CAS NO: | 212631-61-3 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 212631-61-3 |
| 化学名 | N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-((4-iodo-2-methylphenyl)amino)benzamide |
| Canonical SMILES | IC1=CC=C(C(C)=C1)NC(C(C(NOCC2CC2)=O)=CC(F)=C3F)=C3F |
| 分子式 | C18H16F3IN2O2 |
| 分子量 | 476.23 |
| 溶解度 | DMSO: 100 mM,Ethanol: 100 mM |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 8 nM for MEK [1] 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 [1]. 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 [1]. 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 [2]. Clinical trial: So far, no clinical study has been conducted. References: |
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