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

444937
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      Overview

      Key Spec Table

      Empirical FormulaCAS #
      C₂₁H₁₈N₄OS297744-42-4

      Pricing & Availability

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      444937-1MG
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          1 mg
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          444937-5MG
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              5 mg
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              Description
              Overview A 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 Number 444937
              Brand Family Calbiochem®
              References
              References Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.
              Product Information
              CAS number 297744-42-4
              ATP Competitive N
              Form White solid
              Hill Formula C₂₁H₁₈N₄OS
              Chemical formula C₂₁H₁₈N₄OS
              Molar Mass 374.5
              Reversible N
              Structure formula Image
              Applications
              Biological Information
              Primary Target MEK
              Primary Target IC<sub>50</sub> 12 nM against MEK
              Purity ≥ 95% by HPLC (sum of two isomers)
              Physicochemical Information
              Cell permeable Y
              Solubility DMSO or MeOH
              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 No
              Special Instructions Following 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

              MSDS

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              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.

              Revision 13-April-2011 RFH
              Description A 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.).
              Form White solid
              Intert gas (Yes/No) Packaged under inert gas
              CAS number 297744-42-4
              Molar mass 374.5
              Chemical formula C₂₁H₁₈N₄OS
              Structure formula
              Purity ≥ 95% by HPLC (sum of two isomers)
              Solubility DMSO (10 mg/ml) or Methanol (50 mg/ml)
              Storage -20°C
              Protect from light
              Do Not Freeze No
              Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
              Toxicity Standard Handling
              References Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett. 14, 1483.