448103 | Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor - CAS 888719-03-7 - Calbiochem

448103
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₁₆F₂N₄O₃ 888719-03-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      448103-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA cell-permeable pyrrolopyridine-pyridone compound that acts as a potent ATP-competitive inhibitor of Met, Flt-3 and VEGFR2 (IC50 = 1.9, 4.0 and 27 nM, respectively), while exhibiting much reduced potency against Lck and c-Kit (IC50 = 290 and 610 nM, respectively) and little or no activity agaisnt Cdk2/CycE, IGF-1R, InsR, MK-2, PKA, and PKCα (IC50 >1 µM). Shown to selectively inhibit the Met-dependent, but not Met-independent, proliferation of gastric carcinoma cultures (IC50 = 60 nM vs. >5 µM against GTL-6 and N87 cells, respectively) in vitro and effectively abolish GTL-6-derived tumor growth (110% reduction of control tumor mass 39 days after tumor implant) by daily oral dosing (50 mg/kg) in mice in vivo.
          Catalogue Number448103
          Brand Family Calbiochem®
          SynonymsN-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, Flt-3 Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXVI, VEGFR2 Kinase Inhibitor XXIV
          References
          ReferencesKim, K.S., et al. 2008. J. Med. Chem. 51, 5330.
          Product Information
          CAS number888719-03-7
          FormWhite solid
          Hill FormulaC₂₅H₁₆F₂N₄O₃
          Chemical formulaC₂₅H₁₆F₂N₄O₃
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% 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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          448103

          References

          Reference overview
          Kim, K.S., et al. 2008. J. Med. Chem. 51, 5330.
          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.

          Revision13-April-2011 RFH
          SynonymsN-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, Flt-3 Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXVI, VEGFR2 Kinase Inhibitor XXIV
          DescriptionA cell-permeable pyrrolopyridine-pyridone compound that acts as a potent ATP-competitive inhibitor of Met, Flt-3 and VEGFR2 (IC50 = 1.9, 4.0 and 27 nM, respectively), while exhibiting much reduced potency against Lck and c-Kit (IC50 = 290 and 610 nM, respectively) and little or no activity agaisnt Cdk2/CycE, IGF-1R, InsR, MK-2, PKA, and PKCα (IC50 >1 µM). Shown to selectively inhibit the Met-dependent, but not Met-independent, proliferation of gastric carcinoma cultures (IC50 = 60 nM vs. >5 µM against GTL-6 and N87 cells, respectively) in vitro and effectively abolish GTL-6-derived tumor growth (110% reduction of control tumor mass 39 days after tumor implant) by daily oral dosing (50 mg/kg) in mice in vivo.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number888719-03-7
          Chemical formulaC₂₅H₁₆F₂N₄O₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (10 mg/ml) or Ethanol (1 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesKim, K.S., et al. 2008. J. Med. Chem. 51, 5330.