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676483 VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII

Primary Target: VEGFR
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      Overview

      Replacement Information

      Key Specifications Table

      CAS #Empirical Formula
      475108-18-0C₂₂H₁₉ClN₄O₅ • H₂O
      Description
      Overview

      This product has been discontinued.



      A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC50 = 30, 6.5, and 15 nM for VEGFR-1,-2,and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC50 = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.
      Catalogue Number676483
      Brand Family Calbiochem®
      SynonymsVascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII
      References
      ReferencesNakamura, K., et al. 2006. Cancer Res. 66, 9134.
      Product Information
      CAS number475108-18-0
      ATP CompetitiveN
      FormPink solid
      Hill FormulaC₂₂H₁₉ClN₄O₅ • H₂O
      Chemical formulaC₂₂H₁₉ClN₄O₅ • H₂O
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetVEGFR
      Primary Target IC<sub>50</sub>30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively; 24, 40, 49, 78, and 78 nM for EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2, respectively
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalog Number GTIN
      676483 0

      Documentation

      VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      676483

      References

      Reference overview
      Nakamura, K., et al. 2006. Cancer Res. 66, 9134.

      Brochure

      Title
      Biologics 33.2
      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.

      Revision19-April-2011 RFH
      SynonymsVascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII
      DescriptionA cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC50 = 30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC50 = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.
      FormPink solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number475108-18-0
      Chemical formulaC₂₂H₁₉ClN₄O₅ • H₂O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage Protect from light
      +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
      ReferencesNakamura, K., et al. 2006. Cancer Res. 66, 9134.