194975 B-Cell Immunosuppressant

194975
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₆H₁₀F₃N₃O 237067-55-9
      Description
      Overview

      This product has been discontinued.





      A cell-permeable quinolinecarboxamide that acts as a potent and highly selective B-cell immunosuppressant with a 75-fold selectivity for B- over T-cells and no general cytotoxicity. Does not affect DHO- and IMP-dehydrogenases, or the kinase activities of EGFR, PDGFR, Cdk2, and Src (IC50 > 30 µM). Shown to effectively block TI (T-cell signal independent) Ab production in vivo (ED50 ≤ 3 mg/kg/day, administered subcutaneously or orally in mice). It is ~100-fold superior to Leflunomide (0.3 mg/kg/day v.s. 50mg/kg/day, respectively) in suppressing Ab-mediated xenograft rejection in a mouse xenotransplantation model.
      Catalogue Number194975
      Brand Family Calbiochem®
      SynonymsN-[5-(Trifluoromethyl)pyridin-2-yl]quinole-8-carboxamide
      References
      ReferencesPapageorgiou, C., et al. 2001. J. Med. Chem. 44, 1986.
      Product Information
      CAS number237067-55-9
      FormWhite solid
      Hill FormulaC₁₆H₁₀F₃N₃O
      Chemical formulaC₁₆H₁₀F₃N₃O
      Structure formula ImageStructure formula Image
      Applications
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°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.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      MSDS

      Title

      Safety Data Sheet (SDS) 

      Certificates of Analysis

      TitleLot Number
      194975

      References

      Reference overview
      Papageorgiou, C., et al. 2001. J. Med. Chem. 44, 1986.
      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.

      Revision05-April-2011 RFH
      SynonymsN-[5-(Trifluoromethyl)pyridin-2-yl]quinole-8-carboxamide
      DescriptionA cell-permeable, potent, and highly selective B-cell immunosuppressant with 75-fold greater selectivity for B-cells compared to T-cells, with no general cytotoxic effects. Does not affect DHO- and IMP-dehydrogenases, or EGFR, PDGFR, Cdk2, and Src kinase activities (IC50 >30 µM). Reported to effectively block T-cell signal independent (TI) antibody(Ab) production in mice (ED50 <3 mg/kg/day, administered subcutaneously or orally). Shown to be ~100-fold more effective that Leflunomide (0.3 mg/kg/day vs. 50 mg/kg/day, respectively) in suppressing Ab-mediated xenograft rejection in a mouse xenotransplantation model.
      FormWhite solid
      CAS number237067-55-9
      Chemical formulaC₁₆H₁₀F₃N₃O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (25 mg/ml) or Methanol (5 mg/ml)
      Storage +2°C to +8°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
      ReferencesPapageorgiou, C., et al. 2001. J. Med. Chem. 44, 1986.