572888 SU1498 - Calbiochem

572888
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₅H₃₀N₂O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      572888-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC50 = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Also reduces the expression of ets-1, a transcription factor stimulated by VEGF. Has only a weak inhibitory effect on PDGF-receptor (IC50 >50 µM), EGF-receptor (IC50 >100 µM), and HER2 (IC50 >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay.
          Catalogue Number572888
          Brand Family Calbiochem®
          Synonyms(E)-3-(3,5-Diisopropyl-4-hydroxyphenyl)-2-[(3-phenyl-n-propyl)amino-carbonyl]acrylonitrile, VEGFR Tyrosine Kinase Inhibitor VIII, VEGFR2 Kinase Inhibitor X
          References
          ReferencesArbiser, J.L., et al. 2000. Am. J. Pathol. 156, 1469.
          Strawn, L.M., et al. 1996. Cancer Res. 56, 3540.
          Product Information
          ATP CompetitiveY
          FormPale yellow solid
          Hill FormulaC₂₅H₃₀N₂O₂
          Chemical formulaC₂₅H₃₀N₂O₂
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          ApplicationSU1498, CAS 168835-82-3, is a potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC50 = 700 nM).
          Biological Information
          Primary TargetFlk-1 kinase
          Primary Target IC<sub>50</sub>700 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 -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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SU1498 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          SU1498 - Calbiochem Certificates of Analysis

          TitleLot Number
          572888

          References

          Reference overview
          Arbiser, J.L., et al. 2000. Am. J. Pathol. 156, 1469.
          Strawn, L.M., et al. 1996. Cancer Res. 56, 3540.

          Citations

          Title
        • Marie Dance, et al. (2006) The adaptor protein gab1 couples the stimulation of vascular endothelial growth factor receptor-2 to the activation of phosphoinositide 3-kinase. Journal of Biological Chemistry 281, 23285-23295.
        • Ursula Mayr, et al. (2006) Accelerated Arteriosclerosis of Vein Grafts in Inducible NO Synthase-/- Mice Is Related to Decreased Endothelial Progenitor Cell Repair. Circulation Research 98, 412-420.
        • Meenalakshmi M. Mariappan, et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
        • Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618.
        • 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.

          Revision12-January-2010 RFH
          Synonyms(E)-3-(3,5-Diisopropyl-4-hydroxyphenyl)-2-[(3-phenyl-n-propyl)amino-carbonyl]acrylonitrile, VEGFR Tyrosine Kinase Inhibitor VIII, VEGFR2 Kinase Inhibitor X
          DescriptionA potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC50 = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Has only a weak inhibitory effect on PDGF receptor (IC50 >50 µM), EGF-receptor (IC50 >100 µM), and HER-2 (IC50 >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay.
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₅H₃₀N₂O₂
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (5 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesArbiser, J.L., et al. 2000. Am. J. Pathol. 156, 1469.
          Strawn, L.M., et al. 1996. Cancer Res. 56, 3540.
          Citation
        • Marie Dance, et al. (2006) The adaptor protein gab1 couples the stimulation of vascular endothelial growth factor receptor-2 to the activation of phosphoinositide 3-kinase. Journal of Biological Chemistry 281, 23285-23295.
        • Ursula Mayr, et al. (2006) Accelerated Arteriosclerosis of Vein Grafts in Inducible NO Synthase-/- Mice Is Related to Decreased Endothelial Progenitor Cell Repair. Circulation Research 98, 412-420.
        • Meenalakshmi M. Mariappan, et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
        • Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618.