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676489 VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem

676489
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₇H₁₃N₃OS 216661-57-3
      Description
      Overview

      This product has been discontinued.





      A 3,6-diaryl substituted pyrazolopyrimidine that acts as a potent, reversible, and ATP-competitive inhibitor of VEGFR-2 (KDR/Flk-1; IC50 = 19 nM). Displays ~2-fold greater selectivity for VEGFR-2 over PDGFRβ (IC50 = 34 nM) and 10-fold greater selectivity over VEGFR-1 (Flt-1) and VEGFR-3 (Flt-4; IC50 = 190 nM) tyrosine kinase activity. Does not inhibit FGFR-1 or Src kinase activity (IC50 > 1.9 µM). Shown to inhibit VEGF-stimulated mitogenesis in human umbilical vein endothelial cells (IC50 = 387 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.
      Catalogue Number676489
      Brand Family Calbiochem®
      SynonymsKDR/Flk-1 Kinase Inhibitor IV, 3-(3-Thienyl)-6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidine, Vascular Endothelial Growth FactorReceptor 2 Kinase Inhibitor IV, VEGFR Tyrosine Kinase Inhibitor XVIII, VEGFR1 Kinase Inhibitor II, VEGFR3 Kinase Inhibitor II, PDGFR Tyrosine Kinase Inhibitor IX
      References
      ReferencesCools, J., et al. 2004. Cancer Res. 64, 6385.
      Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.
      Product Information
      CAS number216661-57-3
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₁₇H₁₃N₃OS
      Chemical formulaC₁₇H₁₃N₃OS
      ReversibleY
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary TargetVEGFR-2 KDR/Flk-1
      Primary Target IC<sub>50</sub>19 nM
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableN
      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 Standard Handling
      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

      VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      676489

      References

      Reference overview
      Cools, J., et al. 2004. Cancer Res. 64, 6385.
      Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.
      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.

      Revision13-January-2010 RFH
      SynonymsKDR/Flk-1 Kinase Inhibitor IV, 3-(3-Thienyl)-6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidine, Vascular Endothelial Growth FactorReceptor 2 Kinase Inhibitor IV, VEGFR Tyrosine Kinase Inhibitor XVIII, VEGFR1 Kinase Inhibitor II, VEGFR3 Kinase Inhibitor II, PDGFR Tyrosine Kinase Inhibitor IX
      DescriptionA 3,6-diaryl substituted pyrazolopyrimidine that acts as a potent, reversible, and ATP-competitive inhibitor of vascular endothelial cell growth factor receptor-2 (VEGFR-2; KDR/Flk-1) (IC50 = 19 nM). Displays ~2-fold greater selectivity for VEGFR-2 compared to platelet derived growth factor receptor β (PDGFRβ) and 10-fold selectivity compared to VEGFR-1 (Flt-1) and VEGFR-3 (Flt-4). Does not inhibit FGFR-1 or Src kinase activity. Reported to inhibit VEGF-stimulated mitogenesis in human umbilical vein endothelial cells (IC50 = 387 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number216661-57-3
      Chemical formulaC₁₇H₁₃N₃OS
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 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 Standard Handling
      ReferencesCools, J., et al. 2004. Cancer Res. 64, 6385.
      Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.