538776 FGFR4 Inhibitor, BLU9931 - Calbiochem

538776
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₆H₂₂Cl₂N₄O₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38776.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable anilinoquinazoline derivative that acts as a highly potent, irreversible, paralog selective inhibitor of fibroblast growth factor receptor 4 kinase (FGFR4; IC50 = 3 nM; kinact/KI = 0.6 x 105 (mol/L) -1s-1). Acts by forming a covalent bond with Cys552 within the ATP-binding pocket of FGFR4. Has minimal effect on FGFR1, 2, and 3 (IC50 = 591 nM, 493 nM, and 150 nM respectively) and does not display any activity towards a panel of 455 other protein kinases. Suppresses FGFR4 signaling and phosphorylation of downstream components in MDA-MB-453 cells. Also shown to be a potent inhibitor of downstream signaling in Hep 3B hepatocellular carcinoma (HCC) cells expressing FGF19 and induces caspase 3 and 7 activity. Inhibits the growth of Hep 3B HCC xenografts in murine model (100 mg/kg, b.i.d; p.o. for 21 days). Displays desirable pharmacokinetic properties with moderate bioavailability (18%) and t1/2 = 2.3 h (~ 10 mg/kg, p.o.).
          Catalogue Number538776
          Brand Family Calbiochem®
          SynonymsFibroblast Growth Factor Receptor 4 Inhibitor, BLU9931
          References
          ReferencesHagel, M., et al. 2015. Cancer Discov. 5, 424.
          Product Information
          FormOff-white solid
          Hill FormulaC₂₆H₂₂Cl₂N₄O₃
          Chemical formulaC₂₆H₂₂Cl₂N₄O₃
          ReversibleN
          Applications
          Biological Information
          Primary TargetFGFR4
          Primary Target IC<sub>50</sub>3 nM
          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
          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

          FGFR4 Inhibitor, BLU9931 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Hagel, M., et al. 2015. Cancer Discov. 5, 424.
          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.

          Revision28-July-2017 JSW
          SynonymsFibroblast Growth Factor Receptor 4 Inhibitor, BLU9931
          DescriptionA cell-permeable anilinoquinazoline derivative that acts as a highly potent, irreversible, paralog selective inhibitor of fibroblast growth factor receptor 4 kinase (FGFR4; IC50 = 3 nM; kinact/KI = 0.6 x 105 (mol/L) -1s-1). Acts by forming a covalent bond with Cys552 within the ATP-binding pocket of FGFR4. Has minimal effect on FGFR1, 2, and 3 (IC50 = 591 nM, 493 nM, and 150 nM respectively) and does not display any activity towards a panel of 455 other protein kinases. Suppresses FGFR4 signaling and phosphorylation of downstream components in MDA-MB-453 cells. Also shown to be a potent inhibitor of downstream signaling in Hep 3B hepatocellular carcinoma (HCC) cells expressing FGF19 and induces caspase 3 and 7 activity. Inhibits the growth of Hep 3B HCC xenografts in murine model (100 mg/kg, b.i.d; p.o. for 21 days). Displays desirable pharmacokinetic properties with moderate bioavailability (18%) and t1/2 = 2.3 h (~ 10 mg/kg, p.o.).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₆H₂₂Cl₂N₄O₃
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -20°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
          ReferencesHagel, M., et al. 2015. Cancer Discov. 5, 424.