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100128 A77 1726 - CAS 108605-62-5 - Calbiochem

100128
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₁₂H₉F₃N₂O₂108605-62-5

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100128-5MG
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      Plastic ampoule 5 mg
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      Description
      OverviewLeflunomide metabolite that blocks TNF-dependent NF-κB activation and gene expression. Inhibits the activity of dihydroorotate dehydrogenase (DHO-DH; IC50 = 220 nM). Reported to reduce IFN-γ-induced expression of iNOS in L929 fibroblasts. Inhibits IL-1β-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells. A cell-permeable, reversible, and substrate competitive inhibitor that inhibits the IL-2-induced tyrosine phosphorylation of JAK1 and JAK3.
      Catalogue Number100128
      Brand Family Calbiochem®
      SynonymsN-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide
      References
      ReferencesJankovic, V., et al. 2000. Cell Immunol. 199, 73.
      Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589.
      Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095.
      Elder, R.T., et al. 1997. J. Immunol. 159, 22.
      Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527.
      Xu, X., et al. 1995. J. Biol. Chem. 270, 12398.
      Mattar, T., et al. 1993. FEBS Lett. 334, 161.
      Product Information
      CAS number108605-62-5
      ATP CompetitiveN
      FormWhite solid
      Hill FormulaC₁₂H₉F₃N₂O₂
      Chemical formulaC₁₂H₉F₃N₂O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetDihydroorotate dehydrogenase (DHO-DH)
      Primary Target IC<sub>50</sub>220 nM against DHO-DH
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 40

      Limited evidence of a carcinogenic effect.
      S PhraseS: 22-36

      Do not breathe dust.
      Wear suitable protective clothing.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Carcinogenic / Teratogenic
      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

      A77 1726 - CAS 108605-62-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      100128

      References

      Reference overview
      Jankovic, V., et al. 2000. Cell Immunol. 199, 73.
      Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589.
      Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095.
      Elder, R.T., et al. 1997. J. Immunol. 159, 22.
      Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527.
      Xu, X., et al. 1995. J. Biol. Chem. 270, 12398.
      Mattar, T., et al. 1993. FEBS Lett. 334, 161.
      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.

      Revision11-January-2010 RFH
      SynonymsN-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide
      DescriptionLeflunomide metabolite that blocks TNF-dependent NF-κB activation and gene expression. Inhibits the activity of dihydroorotate dehydrogenase (DHO-DH; IC50 = 220 nM). Reported to reduce IFN-γ-induced expression of iNOS in L929 fibroblasts. Inhibits IL-1β-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells.A cell-permeable, reversible and substrate competitive inhibitor that inhibits the IL-2-induced tyrosine phosphorylation of JAK1 and JAK3.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number108605-62-5
      Chemical formulaC₁₂H₉F₃N₂O₂
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (35 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 Carcinogenic / Teratogenic
      ReferencesJankovic, V., et al. 2000. Cell Immunol. 199, 73.
      Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589.
      Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095.
      Elder, R.T., et al. 1997. J. Immunol. 159, 22.
      Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527.
      Xu, X., et al. 1995. J. Biol. Chem. 270, 12398.
      Mattar, T., et al. 1993. FEBS Lett. 334, 161.