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3B Pharmachem (Wuhan) International Co.,Ltd.
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Product Name:PD 198306;N-(CyclopropylMethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-Methylphenyl)aMino]-benzaMide
CAS:212631-61-3
Purity:99% HPLC Package:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
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BOC Sciences
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Product Name:PD 198306
CAS:212631-61-3
Purity:98% by HPLC Remarks:PD 198306, an amino-benzamide compound, is an orally bioavailable and potent inhibitor of MAPK kinase 1/2 (MEK1/2; IC50 = 8 nM). It inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK
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EMMX Biotechnology LLC
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Product Name:PD 198306
CAS:212631-61-3
Purity:98% HPLC Package:5mg;10mg;25mg;50mg;100mg;250mg;500mg;1g
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Tianjin Kailiqi Biotechnology Co., Ltd.
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Product Name:PD198306
CAS:212631-61-3
Purity:大于98% Package:1g,5g,10g,25g根据客户需要分装 Remarks:Not For Human Use, Lab Use Only.
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| | N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Basic information |
| Product Name: | N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE | | Synonyms: | 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 | | CAS: | 212631-61-3 | | MF: | C18H16F3IN2O2 | | MW: | 476.23 | | EINECS: | | | Product Categories: | | | Mol File: | 212631-61-3.mol | ![N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Structure](CAS/GIF/212631-61-3.gif) |
| | N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Chemical 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 |
| | N-(CYCLOPROPYLMETHOXY)-3,4,5-TRIFLUORO-2-[(4-IODO-2-METHYLPHENYL)AMINO]-BENZAMIDE Usage And Synthesis |
| 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 |
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