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444968 InSolution™ MEK1/2 Inhibitor III, PD0325901 - CAS 391210-10-9 - Calbiochem

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
391210-10-9C₁₆H₁₄F₃IN₂O₄

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444968-5MGCN
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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.
      Catalogue Number444968
      Brand Family Calbiochem®
      SynonymsPD 0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD325901
      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
      FormLiquid
      FormulationA 50 mM (5 mg/207 µl) solution of MEK1/2 Inhibitor III, PD0325901 (Cat. No. 444966) in DMSO.
      Hill FormulaC₁₆H₁₄F₃IN₂O₄
      Chemical formulaC₁₆H₁₄F₃IN₂O₄
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationInSolution™ MEK1/2 Inhibitor III, PD0325901, CAS 391210-10-9, is a 50 mM solution of MEK1/2 Inhibitor III, PD0325901 in DMSO. A cell-permeable, potent, non-competitive MEK/MAPKK/MKK inhibitor.
      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 Dry Ice Only
      Toxicity Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      444968-5MGCN 04055977204544

      Documentation

      InSolution™ MEK1/2 Inhibitor III, PD0325901 - CAS 391210-10-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      InSolution™ MEK1/2 Inhibitor III, PD0325901 - CAS 391210-10-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      444968

      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.

      Brochure

      Title
      New Products: Volume 3, 2012
      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.

      Revision03-April-2012 JSW
      SynonymsPD 0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD325901
      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.
      FormLiquid
      FormulationA 50 mM (5 mg/207 µl) solution of MEK1/2 Inhibitor III, PD0325901 (Cat. No. 444966) in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number391210-10-9
      Chemical formulaC₁₆H₁₄F₃IN₂O₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      Storage Protect from light
      -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
      Toxicity Regulatory Review
      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.