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504981 Tie2/Trk Dual Inhibitor - Calbiochem

Tie2/Trk Dual Inhibitor - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: Tie2 Inhibitor IV, Trk Inhibitor VII

Primary Target: TrkA
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      Übersicht

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₃H₂₁ClN₆O₂
      Description
      Overview

      This product has been discontinued.



      A cell-permeable pyrrolopyrimidinyl-phenyl urea that acts as a potent, reversible, ATP-competitive inhibitor against Tie2 and TrkA kinase activity in cell-free assays (IC50 = 40 and 0.4 nM, respectively; [ATP] = 100 µM) as well as Tie2- and TrkA-dependent tyrosine phosphorylation of cellular proteins upon ligand stimulation in cultures (IC50 = 3.7 and 4 nM, with respective NIH 3T3 transfectant), displaying much reduced potency against PDGFR (IC50 =1.4 µM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC50 >10 µM). Reported to be efficacious in suppressing rat C6 glioblastoma tumor expansion (10 to 33 mg/kg/d, or 10 mg/kg/12 h p.o.) in vivo.
      Catalogue Number504981
      Brand Family Calbiochem®
      SynonymsTie2 Inhibitor IV, Trk Inhibitor VII
      References
      ReferencesArcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.
      Product Information
      FormWhite solid
      Hill FormulaC₂₃H₂₁ClN₆O₂
      Chemical formulaC₂₃H₂₁ClN₆O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTrkA
      Secondary targetTie-2
      Purity≥99% 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 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
      Global Trade Item Number
      Bestellnummer GTIN
      504981 0

      Documentation

      Tie2/Trk Dual Inhibitor - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Arcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.
      Datenblatt

      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.

      Revision20-September-2013 JSW
      SynonymsTie2 Inhibitor IV, Trk Inhibitor VII
      DescriptionA cell-permeable pyrrolopyrimidinyl-phenyl urea that acts as a potent, reversible, ATP-competitive inhibitor against Tie2 and TrkA kinase activity in cell-free assays (IC50 = 40 and 0.4 nM, respectively; [ATP] = 100 µM) as well as Tie2- and TrkA-dependent tyrosine phosphorylation of cellular proteins upon ligand stimulation in cultures (IC50 = 3.7 and 4 nM, respectively, using respective NIH 3T3 transfectant; 1 h drug preincubation), displaying much reduced potency against PDGFR (IC50 =1.4 µM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC50 >10 µM). Reported to be orally available in rat (systemic Cmax = 1,715 ng/mL; Tmax = 0.75 h; 4.2 mg/kg p.o. using ultrafasted rats) and efficacious in suppressing rat C6 glioblastoma tumor expansion (by 40%, 60%, and 70% in 10 d, respectively, with 10 mg/kg/d, 33 mg/kg/d, or 10 mg/kg/12 h oral dosing schedule) in vivo.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₃H₂₁ClN₆O₂
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesArcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.