444966
MEK1/2 Inhibitor III
The MEK1/2 Inhibitor III, also referenced under CAS 391210-10-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonyme(s) :
MEK1/2 Inhibitor III, PD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III
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About This Item
Formule empirique (notation de Hill):
C16H14F3IN2O4
Numéro CAS:
Poids moléculaire :
482.19
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produits recommandés
Niveau de qualité
Pureté
≥95% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
white to off-white
Solubilité
DMSO: 20 mg/mL
Conditions d'expédition
ambient
Température de stockage
2-8°C
InChI
1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1
Clé InChI
SUDAHWBOROXANE-SECBINFHSA-N
Description générale
A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo.
A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo. Also available in InSolution format (Cat. No. 444968).
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Autres remarques
Barrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett.18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther.7, 3112.
Silva, J., et al. 2008. PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008. Nature453, 519.
Bain, J., et al. 2007. Biochem. J.408, 297.
Solit, D.B., et al. 2006. Nature439, 358.
Leyton, J., et al. 2008. Mol. Cancer Ther.7, 3112.
Silva, J., et al. 2008. PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008. Nature453, 519.
Bain, J., et al. 2007. Biochem. J.408, 297.
Solit, D.B., et al. 2006. Nature439, 358.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Mention d'avertissement
Danger
Mentions de danger
Conseils de prudence
Classification des risques
Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2
Code de la classe de stockage
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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