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444937 MEK Inhibitor I - CAS 297744-42-4 - Calbiochemv

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
297744-42-4C₂₁H₁₈N₄OS

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444937-1MG
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      Description
      OverviewA cell-permeable pyridine-containing vinylogous cyanamide compound that acts as a potent and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 > 1 µM). The inhibition is noncompetitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.).
      Catalogue Number444937
      Brand Family Calbiochem®
      References
      ReferencesWityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.
      Product Information
      CAS number297744-42-4
      ATP CompetitiveN
      FormWhite solid
      Hill FormulaC₂₁H₁₈N₄OS
      Chemical formulaC₂₁H₁₈N₄OS
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMEK
      Primary Target IC<sub>50</sub>12 nM against MEK
      Purity≥ 95% by HPLC (sum of two isomers)
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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
      Global Trade Item Number
      Catalog Number GTIN
      444937-1MG 04055977186215

      Documentation

      MEK Inhibitor I - CAS 297744-42-4 - Calbiochemv SDS

      Title

      Safety Data Sheet (SDS) 

      MEK Inhibitor I - CAS 297744-42-4 - Calbiochemv Certificates of Analysis

      TitleLot Number
      444937

      References

      Reference overview
      Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.

      Brochure

      Title
      MAPK Pathway Poster ( 750 KB )
      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.

      Revision13-April-2011 RFH
      DescriptionA cell-permeable, potent, and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 >1 µM). The inhibition is non-competitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. non-competitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number297744-42-4
      Chemical formulaC₂₁H₁₈N₄OS
      Structure formulaStructure formula
      Purity≥ 95% by HPLC (sum of two isomers)
      SolubilityDMSO (10 mg/ml) or Methanol (50 mg/ml)
      Storage Protect from light
      -20°C
      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
      ReferencesWityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.