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521232 PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem

521232
  
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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      205254-94-0C₂₇H₂₇N₅O₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable piperazinyl-quinazoline carboxamide compound that acts as a potent, ATP-competitive, reversible, and selective inhibitor of PDGF receptor family of tyrosine kinases (IC50 = 0.05 µM for α-PDGFR; 0.08 µM for β-PDGFR; 0.05 µM for c-Kit; 0.23 µM for Flt3). Affects the activities of other kinases only at much higher concentrations (IC50 ≥ 30 µM for EGFR, FGFR, Src, PKA & PKC). Reported to block the PDGF-BB induced proliferation of porcine aorta smooth muscle cells (IC50 = 0.25 µM).

      Catalogue Number521232
      Brand Family Calbiochem®
      Synonyms4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide
      References
      ReferencesMatsuno, K., et al. 2003. J. Med. Chem. 46, 4910.
      Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3001.
      Matsuno, K., et al. 2002. J. Med. Chem. 45, 4513.
      Matsuno, K., et al. 2002. J. Med. Chem. 45, 3057.
      Product Information
      CAS number205254-94-0
      ATP CompetitiveY
      FormWhite solid
      Hill FormulaC₂₇H₂₇N₅O₄
      Chemical formulaC₂₇H₂₇N₅O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetα-PDGFR
      Primary Target IC<sub>50</sub>0.05 µM for α-PDGFR; 0.08 µM for β-PDGFR; 0.05 µM for c-Kit; 0.23 µM for Flt3
      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 Carcinogenic / Teratogenic
      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
      Catalogue Number GTIN
      521232 0

      Documentation

      PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      521232

      References

      Reference overview
      Matsuno, K., et al. 2003. J. Med. Chem. 46, 4910.
      Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3001.
      Matsuno, K., et al. 2002. J. Med. Chem. 45, 4513.
      Matsuno, K., et al. 2002. J. Med. Chem. 45, 3057.
      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
      Synonyms4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide
      DescriptionA cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of PDGF receptor family of tyrosine kinases (IC50 = 50 nM for α-PDGFR, 80 nM for β-PDGFR, 50 nM for c-Kit, and 230 nM for Flt3). Inhibits the activities of other kinases only at much higher concentrations (IC50 > 30 µM for EGFR, FGFR, Src, PKA, and PKC). Reported to block PDGF-BB-induced proliferation of porcine aorta smooth muscle cells (IC50 = 250 nM).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number205254-94-0
      Chemical formulaC₂₇H₂₇N₅O₄
      Structure formulaStructure formula
      Purity≥97% 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 Carcinogenic / Teratogenic
      ReferencesMatsuno, K., et al. 2003. J. Med. Chem. 46, 4910.
      Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3001.
      Matsuno, K., et al. 2002. J. Med. Chem. 45, 4513.
      Matsuno, K., et al. 2002. J. Med. Chem. 45, 3057.