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572888 SU1498 - Calbiochem

572888
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₅H₃₀N₂O₂

Products

Catalogue NumberPackaging Qty/Pack
572888-5MG Glass bottle 5 mg
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
Quality LevelMQ100
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
Global Trade Item Number
Catalogue Number GTIN
572888-5MG 04055977266337

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 Protect from light
    -20°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
    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.