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444966 MEK1/2 Inhibitor III - CAS 391210-10-9 - Calbiochem

444966
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Overview

Key Spec Table

CAS #Empirical Formula
391210-10-9C₁₆H₁₄F₃IN₂O₄

Products

Catalogue NumberPackaging Qty/Pack
444966-5MG Plastic ampoule 5 mg
Description
OverviewA 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).
Catalogue Number444966
Brand Family Calbiochem®
SynonymsPD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III
References
ReferencesBarrett, 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. Nature 453, 519.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Solit, D.B., et al. 2006. Nature 439, 358.
Product Information
CAS number391210-10-9
FormWhite to off-white solid
Hill FormulaC₁₆H₁₄F₃IN₂O₄
Chemical formulaC₁₆H₁₄F₃IN₂O₄
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationMEK1/2 Inhibitor III, CAS 391210-10-9, is a cell-permeable, non-competitive, highly potent MEK/MAPKK/MKK inhibitor that blocks cellular Erk1/2 phosphorylation (IC50 = 25 in serum starved HeLa cells).
Biological Information
Purity≥95% by HPLC
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
444966-5MG 04055977204520