219499 CEP-701 - CAS 111358-88-4 - Calbiochem

219499
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O111358-88-4
      Description
      Overview

      This product has been discontinued.



      A cell-permeable indolocarbazole that is reported to inhibit the activity of several tyrosine kinases, including JAK2/3, Flt3, TrkA, Flk1/KDR/VEGFR2, (IC50 = 0.9, 3, 3.4, and 65 nM, respectively, in cell-free kinase assays) and RET, while exhibiting much reduced potency against PKC and PDGFRβ (IC50 = 218 and 773 nM, respectively) and little or no effect towards EGFR, βIRK, FMS, KIT, or Bcr-Abl. CEP-701 is shown to exhibit anti-cancer efficacy in numerous cultures in vitro as well as in murine and rat xenograft models via subcutaneous or oral dosage (10 to 30 mg/kg, b.i.d.) in vivo.

      Catalogue Number219499
      Brand Family Calbiochem®
      SynonymsKT-5555, JAK2 Inhibitor VIII, JAK3 Inhibitor IX, VEGFR Tyrosine Kinase Inhibitor XXXIII, VEGFR2 Kinase Inhibitor XXXI, PDGFR Tyrosine Kinase Inhibitor XX
      References
      ReferencesHexner, E.O., et al. 2008. Blood 111, 5663.
      Strock, C.J., 2003. Cancer Res. 63, 5559.
      Zheng, R., et al. 2002. Blood 100, 4154.
      Levis, M., et al. 2002. Blood 99, 3885.
      Miknyoczki, S.J., et al. 1999. Clin. Cancer Res. 5, 2205.
      Miknyoczki, S.J., et al. 1999. Ann. N.Y. Acad. Sci. 880, 252.
      George, D.J., et al. 1999. Cancer Res. 59, 2395.
      Product Information
      CAS number111358-88-4
      FormOff-white solid
      Hill FormulaC₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
      Chemical formulaC₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 Ambient Temperature Only
      Toxicity Regulatory Review
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      CEP-701 - CAS 111358-88-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      219499

      References

      Reference overview
      Hexner, E.O., et al. 2008. Blood 111, 5663.
      Strock, C.J., 2003. Cancer Res. 63, 5559.
      Zheng, R., et al. 2002. Blood 100, 4154.
      Levis, M., et al. 2002. Blood 99, 3885.
      Miknyoczki, S.J., et al. 1999. Clin. Cancer Res. 5, 2205.
      Miknyoczki, S.J., et al. 1999. Ann. N.Y. Acad. Sci. 880, 252.
      George, D.J., et al. 1999. Cancer Res. 59, 2395.
      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.

      Revision15-July-2010 RFH
      SynonymsKT-5555, JAK2 Inhibitor VIII, JAK3 Inhibitor IX, VEGFR Tyrosine Kinase Inhibitor XXXIII, VEGFR2 Kinase Inhibitor XXXI, PDGFR Tyrosine Kinase Inhibitor XX
      DescriptionA cell-permeable indolocarbazole that is reported to inhibit the activity of several tyrosine kinases, including JAK2/3, Flt3, TrkA, Flk1/KDR/VEGFR2, (IC50 = 0.9, 3, 3.4, and 65 nM, respectively, in cell-free kinase assays) and RET, while exhibiting much reduced potency against PKC and PDGFRβ (IC50 = 218 and 773 nM, respectively) and little or no effect towards EGFR, βIRK, FMS, KIT, or Bcr-Abl. CEP-701 is shown to exhibit anti-cancer efficacy in numerous cultures in vitro as well as in murine and rat xenograft models via subcutaneous or oral dosage (10 to 30 mg/kg, b.i.d.) in vivo.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number111358-88-4
      Chemical formulaC₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (1 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 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesHexner, E.O., et al. 2008. Blood 111, 5663.
      Strock, C.J., 2003. Cancer Res. 63, 5559.
      Zheng, R., et al. 2002. Blood 100, 4154.
      Levis, M., et al. 2002. Blood 99, 3885.
      Miknyoczki, S.J., et al. 1999. Clin. Cancer Res. 5, 2205.
      Miknyoczki, S.J., et al. 1999. Ann. N.Y. Acad. Sci. 880, 252.
      George, D.J., et al. 1999. Cancer Res. 59, 2395.