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538776 FGFR4 Inhibitor, BLU9931 - Calbiochem

Overview

Key Spec Table

Empirical Formula
C₂₆H₂₂Cl₂N₄O₃

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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
      Quality LevelMQ100
      Biological Information
      Primary TargetFGFR4
      Primary Target IC<sub>50</sub>3 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.38776.0001 04054839119750