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

448103
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₂₅H₁₆F₂N₄O₃ 888719-03-7

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448103-5MGCN
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      塑膠安瓿;塑膠針藥瓶 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 to beige solid
      Hill FormulaC₂₅H₁₆F₂N₄O₃
      Chemical formulaC₂₅H₁₆F₂N₄O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      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

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

      Title

      Safety Data Sheet (SDS) 

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

      Revision14-June-2019 JSW
      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 to beige 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.