N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE
- Product Name
- 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
- Synonyms
- 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
- 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
N-Bromosuccinimide Price
- Product number
- 444965
- Product name
- MEK Inhibitor VIII - CAS 212631-61-3 - Calbiochem
- Packaging
- 5mg
- Price
- $322
- Updated
- 2023/01/07
- Product number
- 23966
- Product name
- PD 198306
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $67
- Updated
- 2024/03/01
- Product number
- 23966
- Product name
- PD 198306
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $231
- Updated
- 2024/03/01
- Product number
- 23966
- Product name
- PD 198306
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $362
- Updated
- 2024/03/01
- Product number
- 2605
- Product name
- PD198306
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $320
- Updated
- 2021/12/16
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
Preparation Products
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