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

219499
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O 111358-88-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      219499-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA 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, VEGFR Tyrosine Kinase Inhibitor XXXIII, VEGFR2 Kinase Inhibitor XXXI, JAK2 Inhibitor VIII, JAK3 Inhibitor IX, 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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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, VEGFR Tyrosine Kinase Inhibitor XXXIII, VEGFR2 Kinase Inhibitor XXXI, JAK2 Inhibitor VIII, JAK3 Inhibitor IX, 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.