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

444937
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₂₁H₁₈N₄OS297744-42-4

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      444937-1MG
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          Plastic ampoule 1 mg
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          444937-5MG
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              Plastic ampoule 5 mg
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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 Image
              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

              Documentation

              SDS

              Title

              Safety Data Sheet (SDS) 

              Certificates of Analysis

              TitleLot Number
              444937

              References

              Reference overview
              Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.
              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 formula
              Purity≥ 95% by HPLC (sum of two isomers)
              SolubilityDMSO (10 mg/ml) or Methanol (50 mg/ml)
              Storage -20°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
              ReferencesWityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.