197221 | Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem

197221
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      Empirical FormulaCAS #
      C₁₈H₁₃F₃N₄O₂ 778270-11-4

      Prix & Disponibilité

      RéférenceDisponibilité Conditionnement Qté Prix Quantité
      197221-5MG
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      Disponibilité limitéeDisponibilité limitée
      En stock 
      Interrompu(e)
      Disponible en quantités limitées
      Disponibilité à confirmer
        Pour le restant : Nous vous tiendrons informé
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          Ampoule plast. 5 mg
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          Description
          OverviewA cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays.
          Catalogue Number197221
          Brand Family Calbiochem®
          Synonyms(3-(6)-(4-Trifluoromethoxy-phenylamino)-pyrimidin-4-yl)-benzamide, GNF-2, Abl Inhibitor I
          References
          ReferencesZhang, J., et al. 2010. Nature 463, 501.
          Choi, Y., et al. 2009. J. Biol. Chem. 284, 29005.
          Adrian, F.J., et al. 2006. Nat. Chem. Biol. 2, 95.
          Product Information
          CAS number778270-11-4
          ATP CompetitiveN
          FormWhite solid
          Hill FormulaC₁₈H₁₃F₃N₄O₂
          Chemical formulaC₁₈H₁₃F₃N₄O₂
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetBcr-abl-expressing cells in Ba/F3.p210
          Primary Target IC<sub>50</sub>138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively
          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 Irritant
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          FDS

          Titre

          Fiche de données de sécurité des matériaux (FDS) 

          Certificats d'analyse

          TitreNuméro de lot
          197221

          Références bibliographiques

          Aperçu de la référence bibliographique
          Zhang, J., et al. 2010. Nature 463, 501.
          Choi, Y., et al. 2009. J. Biol. Chem. 284, 29005.
          Adrian, F.J., et al. 2006. Nat. Chem. Biol. 2, 95.
          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.

          Revision25-March-2010 RFH
          Synonyms(3-(6)-(4-Trifluoromethoxy-phenylamino)-pyrimidin-4-yl)-benzamide, GNF-2, Abl Inhibitor I
          DescriptionA cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number778270-11-4
          Chemical formulaC₁₈H₁₃F₃N₄O₂
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (10 mg/ml) or Ethanol (2 mg/ml)
          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 stable for up to 6 months at -20°C.
          Toxicity Irritant
          ReferencesZhang, J., et al. 2010. Nature 463, 501.
          Choi, Y., et al. 2009. J. Biol. Chem. 284, 29005.
          Adrian, F.J., et al. 2006. Nat. Chem. Biol. 2, 95.