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676487 VEGFR2 Kinase Inhibitor III - CAS 204005-46-9 - Calbiochem

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Synonymes: 3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV

Primary Target: VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      204005-46-9C₁₅H₁₄N₂O
      Description
      Overview

      This product has been discontinued.



      A cell-permeable indolinone compound that acts as a selective, reversible, and ATP-competitive inhibitor of VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases (IC50 = 1.04 µM and 20 µM in NIH 3T3 cells overexpressing Flk-1; Km = 530 nM for ATP). Also potently inhibits the proliferation of HUVECs induced by VEGF, bFGF, or ECGS (IC50 = 50 nM, 5.3 µM and 30.5 µM, respectively). Blocks the autophosphorylation of internal tandem duplication (ITD) and wild type Fms-like tyrosine kinase 3 (FLT3) with an IC50 of 0.1 µM. Does not affect the EGF- or FGF- receptor tyrosine kinases activities even at 100 µM concentration. Reported to induce apoptosis and inhibit VEGF-dependent mitogenesis of human endothelial cells. A 10 mM (500 µg/210 µl) solution of VEGF Receptor 2 Kinase Inhibitor III (Cat. No. 676498) in DMSO is also available.
      Catalogue Number676487
      Brand Family Calbiochem®
      Synonyms3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV
      References
      ReferencesTille, J.C., et al. 2003. Exp. Cell Res. 285, 286.
      Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295.
      Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833.
      Yee, K.W., et al. 2002. Blood 100, 2941.
      Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848.
      Fong, T.A.T., et al. 1999. Cancer Res. 59, 99.
      Sun, L., et al. 1999. J. Med. Chem. 42, 5120.
      Product Information
      CAS number204005-46-9
      ATP CompetitiveY
      FormYellow orange solid
      Hill FormulaC₁₅H₁₄N₂O
      Chemical formulaC₁₅H₁₄N₂O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetVEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases
      Primary Target IC<sub>50</sub>1.04 and 20 µM against VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases, respectively, in NIH 3T3 cells overexpressing Flk-1; ; Km = 530 nM for ATP
      Purity≥97% 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
      Référence GTIN
      676487 0

      Documentation

      VEGFR2 Kinase Inhibitor III - CAS 204005-46-9 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      VEGFR2 Kinase Inhibitor III - CAS 204005-46-9 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      676487

      Références bibliographiques

      Aperçu de la référence bibliographique
      Tille, J.C., et al. 2003. Exp. Cell Res. 285, 286.
      Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295.
      Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833.
      Yee, K.W., et al. 2002. Blood 100, 2941.
      Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848.
      Fong, T.A.T., et al. 1999. Cancer Res. 59, 99.
      Sun, L., et al. 1999. J. Med. Chem. 42, 5120.
      Fiche technique

      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.

      Revision27-September-2010 RFH
      Synonyms3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV
      DescriptionA cell-permeable, selective, reversible, and ATP-competitive inhibitor of VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases (IC50 = 1 µM and 20 µM, respectively in NIH3T3 cells over-expressing Flk-1; Km = 530 nM for ATP). Also reported to potently inhibit the proliferation of HUVECs induced by VEGF, bFGF or ECGS (IC50 = 50 nM, 5.3 µM and 30 µM, respectively). Shown to block the autophosphorylation of internal tandem duplication (ITD) and wild type Fms-like tyrosine kinase 3 (FLT3) (IC50 = 100 nM). Does not affect the activities of EGFR or FGFR tyrosine kinases even at a concentration of 100 µM. Reported to induce apoptosis and inhibit VEGF-dependent mitogenesis of endothelial cells.
      FormYellow orange solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number204005-46-9
      Chemical formulaC₁₅H₁₄N₂O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (5 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
      ReferencesTille, J.C., et al. 2003. Exp. Cell Res. 285, 286.
      Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295.
      Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833.
      Yee, K.W., et al. 2002. Blood 100, 2941.
      Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848.
      Fong, T.A.T., et al. 1999. Cancer Res. 59, 99.
      Sun, L., et al. 1999. J. Med. Chem. 42, 5120.