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504981 | Tie2/Trk Dual Inhibitor - Calbiochem

504981
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₁ClN₆O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04981.0001
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          Glass bottle 10 mg
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          Description
          OverviewA 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 Image
          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

          Documentation

          References

          Reference overview
          Arcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.
          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.

          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 formula
          Purity≥99% 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
          ReferencesArcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.