533434 FGFR Inhibitor, SSR128129E - CAS 848318-25-2 - Calbiochem

533434
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Key Specifications Table

Empirical FormulaCAS #
C₁₈H₁₅N₂O₄Na 848318-25-2

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      Glass bottle 10 mg
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      Description
      OverviewAn orally bioavailable, highly potent allosteric blocker of multi-fibroblast growth factor receptors (FGFR) that specifically binds to the extracellular domain of the receptor and blocks selective responses mediated by FGFR1-4. Does not compete with FGF for binding to FGFR, but inhibits FGF-induced signaling linked to FGFR internalization. Also, does not show any binding to FGF1 or FGF2. Does not affect the activity of other related receptor tyrosine kinases. Shown to block the FGF2-induced ERK1/2 phosphorylation and prevent translocation of FGFR4 from cell surface to the cytosol, but does not block the phosphorylation of VEGFR2 or MET kinase. Inhibits FGF-1-innduced proliferation of HUVEC (IC50= 100 nM) and hB9-myeloma cells (IC50 = 25 nM) and diminishes FGF-2 induced ERK activation in HEKhFGFR2 WT (IC50 = 28 nM). Also reported to reduce the survival of endothelial cells in a dose-dependent manner (IC50 = 17.7 nM). Suppresses the growth of orthotopic Panc02 and 4T1 xenografts in mice (30 mg/kg/day, p.o) and delays the growth of Lewis lung carcinoma. Also shown to be effective against the multi-drug resistant MCF7/ADR breast cancer xenografts. Synergistically enhances the inhibitory effects of anti-VEGFR2.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533434
      Brand Family Calbiochem®
      SynonymsFGFR Inhibitor, SSR
      References
      ReferencesDol-Gleizes, F., et al. 2013. Plos One. 8, e80027.
      Herbert, C., et al. 2013. Cancer Cell. 23, 489.
      Bono. F., et al. 2013. Cancer Cell. 23, 477.
      Product Information
      CAS number848318-25-2
      FormYellow solid
      Hill FormulaC₁₈H₁₅N₂O₄Na
      Chemical formulaC₁₈H₁₅N₂O₄Na
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetFGFR
      Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      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

      FGFR Inhibitor, SSR128129E - CAS 848318-25-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Dol-Gleizes, F., et al. 2013. Plos One. 8, e80027.
      Herbert, C., et al. 2013. Cancer Cell. 23, 489.
      Bono. F., et al. 2013. Cancer Cell. 23, 477.
      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-November-2015 JSW
      SynonymsFGFR Inhibitor, SSR
      DescriptionAn orally bioavailable, highly potent allosteric blocker of multi-fibroblast growth factor receptors (FGFR) that specifically binds to the extracellular domain of the receptor and blocks selective responses mediated by FGFR1-4. Does not compete with FGF for binding to FGFR, but inhibits FGF-induced signaling linked to FGFR internalization. Also, does not show any binding to FGF1 or FGF2. Does not affect the activity of other related receptor tyrosine kinases. Shown to block the FGF2-induced ERK1/2 phosphorylation and prevent translocation of FGFR4 from cell surface to the cytosol, but does not block the phosphorylation of VEGFR2 or MET kinase. Inhibits FGF-1-innduced proliferation of HUVEC (IC50= 100 nM) and hB9-myeloma cells (IC50 = 25 nM) and diminishes FGF-2 induced ERK activation in HEKhFGFR2 WT (IC50 = 28 nM). Also reported to reduce the survival of endothelial cells in a dose-dependent manner (IC50 = 17.7 nM). Suppresses the growth of orthotopic Panc02 and 4T1 xenografts in mice (30 mg/kg/day, p.o) and delays the growth of Lewis lung carcinoma. Also shown to be effective against the multi-drug resistant MCF7/ADR breast cancer xenografts. Synergistically enhances the inhibitory effects of anti-VEGFR2.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number848318-25-2
      Chemical formulaC₁₈H₁₅N₂O₄Na
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°C
      Hygroscopic
      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
      ReferencesDol-Gleizes, F., et al. 2013. Plos One. 8, e80027.
      Herbert, C., et al. 2013. Cancer Cell. 23, 489.
      Bono. F., et al. 2013. Cancer Cell. 23, 477.