197224 Bcr-abl Inhibitor III, GNF-5 - Calbiochem

197224
  
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₁₇F₃N₄O₃
      Description
      OverviewA cell-permeable GNF-2 (Cat. No. 197221) N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 µM against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.
      Catalogue Number197224
      Brand Family Calbiochem®
      SynonymsN-(2-Hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide, Abl Inhibitor III
      References
      ReferencesZhang, J., et al. 2010. Nature 463, 501.
      Product Information
      FormOff-white powder
      Hill FormulaC₂₀H₁₇F₃N₄O₃
      Chemical formulaC₂₀H₁₇F₃N₄O₃
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Bcr-abl Inhibitor III, GNF-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Bcr-abl Inhibitor III, GNF-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      197224

      References

      Reference overview
      Zhang, J., et al. 2010. Nature 463, 501.
      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.

      Revision08-February-2011 RFH
      SynonymsN-(2-Hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide, Abl Inhibitor III
      DescriptionA cell-permeable GNF-2 (Cat. No. 197221) N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 µM against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₇F₃N₄O₃
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml; clear, colorless solution)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesZhang, J., et al. 2010. Nature 463, 501.