ChemicalBook > CAS DataBase List > N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE

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

N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Structure
N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE
  • CAS No.212631-61-3
  • Chemical Name:N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE
  • CBNumber:CB72448962
  • Molecular Formula:C18H16F3IN2O2
  • Formula Weight:476.23
  • MOL File:212631-61-3.mol
N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Property
  • 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
  • FDA UNII WQ5121ZGT3
  • UNSPSC Code 12352200
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Price More Price(1)
  • Brand: Sigma-Aldrich(India)
  • Product number: 444965
  • Product name : MEK Inhibitor VIII - CAS 212631-61-3 - Calbiochem
  • Purity: The MEK1/2 Inhibitor II, also referenced under CAS 212631-61-3, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily
  • Packaging: 5MG
  • Price: ₹20250
  • Updated: 2022/06/14
  • Buy: Buy

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

  • Description 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.
  • Uses PD 198306 is a cell-permeable and highly selective potent inhibitor of MEK 1/2.
  • Definition ChEBI: N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-(4-iodo-2-methylanilino)benzamide is an aminobenzoic acid.
  • Biological Activity 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.
  • 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].
  • IC 50 8 nm for mek [1]
  • storage Store at +4°C
  • References [1] pelletier jp, fernandes jc, brunet j, moldovan f, schrier d, flory c, martel-pelletier j. in vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. arthritis rheum. 2003 jun;48(6):1582-93.
    [2] ciruela a, dixon ak, bramwell s, gonzalez mi, pinnock rd, lee k. identification of mek1 as a novel target for the treatment of neuropathic pain. br j pharmacol. 2003 mar;138(5):751-6.
N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Preparation Products And Raw materials
Raw materials
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N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Spectrum
212631-61-3, N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDERelated Search:
  • 酶
  • 抑制剂
  • C18H16F3IN2O2
  • 化合物PD 198306,10 MM DMSO 溶液
  • PD 198306,MEK1 / 2的抑制剂
  • N-(环丙基甲氧基)-3,4,5-三氟-2-((4-碘-2-甲基苯基)氨基)苯甲酰胺
  • 化合物PD 198306
  • 212631-61-3
  • MEK Inhibitor VIII
  • PD 198306, 10 mM in DMSO
  • 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
  • Benzamide, N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-
  • N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-(4-iodo-2-methylanilino)benzamide
  • PD 198306
  • N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE

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