658551 AG 1296 - CAS 146535-11-7 - Calbiochem

658551
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₁₆H₁₄N₂O₂ 146535-11-7

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658551-5MG
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      Plastic ampoule 5 mg
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      Description
      OverviewSimilar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC50 = 1.0 µM) and β-receptors (IC50 = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC50 of 300 nM and ~1 µM, respectively.
      Catalogue Number658551
      Brand Family Calbiochem®
      Synonyms6,7-Dimethoxy-3-phenylquinoxaline
      References
      ReferencesTse, KF., et al. 2002. Leukemia 16, 2027.
      Tse, KF., et al. 2001. Leukemia 15, 1001.
      Strutz, F., et al. 2001. Kidney Int. 59, 579.
      Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
      Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.
      Product Information
      CAS number146535-11-7
      ATP CompetitiveY
      FormWhite solid
      Hill FormulaC₁₆H₁₄N₂O₂
      Chemical formulaC₁₆H₁₄N₂O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPDGFR kinase
      Primary Target IC<sub>50</sub>1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively
      Purity≥98% 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 -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 1 month at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      AG 1296 - CAS 146535-11-7 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      AG 1296 - CAS 146535-11-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      658551

      References

      Reference overview
      Tse, KF., et al. 2002. Leukemia 16, 2027.
      Tse, KF., et al. 2001. Leukemia 15, 1001.
      Strutz, F., et al. 2001. Kidney Int. 59, 579.
      Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
      Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.
      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
      Synonyms6,7-Dimethoxy-3-phenylquinoxaline
      DescriptionSimilar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC50 = 1.0 µM) and β-receptors (IC50 = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC50 of 300 nM and ~1 µM, respectively.
      FormWhite solid
      CAS number146535-11-7
      Chemical formulaC₁₆H₁₄N₂O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml) or acetonitrile
      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 1 month at -20°C.
      Toxicity Standard Handling
      ReferencesTse, KF., et al. 2002. Leukemia 16, 2027.
      Tse, KF., et al. 2001. Leukemia 15, 1001.
      Strutz, F., et al. 2001. Kidney Int. 59, 579.
      Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
      Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.