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

197221
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₈H₁₃F₃N₄O₂ 778270-11-4

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197221-5MG
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      Ampul plastik 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
      Quality LevelMQ100
      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

      Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      197221

      References

      Reference overview
      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.
      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.

      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.