648451 Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem

648451
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Key Spec Table

Empirical FormulaCAS #
C₂₈H₂₁F₄N₅O₂1033769-28-6

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648451-10MGCN
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      Glass bottle 10 mg
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      Description
      OverviewAn orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50 = 8 and 12 nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC50 = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50 = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50 = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC50 = 3.0 and 5.6 µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.).
      Catalogue Number648451
      Brand Family Calbiochem®
      Synonyms(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
      References
      ReferencesAlbaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press.
      Product Information
      CAS number1033769-28-6
      FormOrange powder
      Hill FormulaC₂₈H₂₁F₄N₅O₂
      Chemical formulaC₂₈H₂₁F₄N₅O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 Ambient Temperature Only
      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 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

      Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem Certificates of Analysis

      TitleLot Number
      648451

      References

      Reference overview
      Albaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press.
      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.

      Revision31-July-2013 JSW
      Synonyms(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
      DescriptionAn orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50 = 8 and 12 nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC50 = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50 = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50 = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC50 = 3.0 and 5.6 µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.).
      FormOrange powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1033769-28-6
      Chemical formulaC₂₈H₂₁F₄N₅O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 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 Standard Handling
      ReferencesAlbaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press.