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

444966
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Key Spec Table

Empirical FormulaCAS #
C₁₆H₁₄F₃IN₂O₄391210-10-9

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444966-5MGCN
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      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
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      MEK1/2 Inhibitor III - CAS 391210-10-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      444966

      References

      Reference overview
      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. Nature 453, 519.
      Bain, J., et al. 2007. Biochem. J. 408, 297.
      Solit, D.B., et al. 2006. Nature 439, 358.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision07-May-2018 JSW
      SynonymsPD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III
      DescriptionA 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.
      FormWhite to off-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number391210-10-9
      Chemical formulaC₁₆H₁₄F₃IN₂O₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (20 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      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.