N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE

 化学構造式
212631-61-3
CAS番号.
212631-61-3
化学名:
别名:
英語名:
N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE
英語别名:
PD 198306;N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-(4-iodo-2-methylanilino)benzamide;N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE;Benzamide, N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-;MAPK,inhibit,neuropathic,Inhibitor,MAP2K,rabies,mitogen-activated protein,drug,MAPKK,PD-198306,phosphatases,PD 198306,inositol,RNA,pain,interference,MEK,ERK,antihyperalgesic,screening,Mitogen-activated protein kinase kinase,phosphate,kinases,PD198306
CBNumber:
CB72448962
化学式:
C18H16F3IN2O2
分子量:
476.23
MOL File:
212631-61-3.mol

N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE 物理性質

融点 :
125-127 °C
比重(密度) :
1.686±0.06 g/cm3(Predicted)
貯蔵温度 :
Store at +4°C
溶解性:
Soluble in DMSO
外見 :
solid
酸解離定数(Pka):
-3.95±0.50(Predicted)
色:
White

安全性情報

N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE 化学特性,用途語,生産方法

説明

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.

使用

PD 198306 is a cell-permeable and highly selective potent inhibitor of MEK 1/2.

生物活性

Potent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30-100 nM. Highly selective for MEK; IC 50 values are > 1, > 4, > 4 and > 10 μ M for ERK, c-Src, cdks and PI 3-kinase γ respectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.

N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE 上流と下流の製品情報

原材料

準備製品


N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE 生産企業

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212631-61-3()キーワード:


  • 212631-61-3
  • N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE
  • PD 198306
  • N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-(4-iodo-2-methylanilino)benzamide
  • Benzamide, N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-
  • MAPK,inhibit,neuropathic,Inhibitor,MAP2K,rabies,mitogen-activated protein,drug,MAPKK,PD-198306,phosphatases,PD 198306,inositol,RNA,pain,interference,MEK,ERK,antihyperalgesic,screening,Mitogen-activated protein kinase kinase,phosphate,kinases,PD198306
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