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531091 Porcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem

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531091
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CAS #Empirical Formula
1243244-14-5C₂₃H₂₀N₆O

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      Description
      OverviewA cell-permeable C59 (Cat. No. 500496) structural analog that potently inhibits Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC50 from 50 pM to 1.1 nM) via direct porcupine (Porcn), but not Wntless, affinity interaction. Shown to inhibit the proliferation of head and neck squamous cell carcinoma (HNSCC) line HN30 (IC50 = 0.3 nM), but not 293T even at a high concentration of 20 µM. In mice & rats receiving therapeutic LGK974 oral dosages (up to 5 mg/10 mL/kg/d), a delayed tissue Wnt signaling suppression (max inhibition 7 to 10 h post dosing) is seen due to pre-existing Wnt in tissue, followed by a full recovery of tissue Wnt signalling at 24 h upon drug clearance. The periodic daily inhibition/recovering cycle is shown to result in tumor regression in mice & rats, while allowing Wnt signaling-dependent normal tissue homeostasis. Overdosing is reported to result in loss of intestinal epithelium in rats receiving 14 consecutive 20 mg/kg daily oral dosages.
      Catalogue Number531091
      Brand Family Calbiochem®
      Synonyms2-(2ʹ,3-Dimethyl-2,4ʹ-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974
      References
      ReferencesLiu, J., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20224.
      Product Information
      CAS number1243244-14-5
      FormTan powder
      Hill FormulaC₂₃H₂₀N₆O
      Chemical formulaC₂₃H₂₀N₆O
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetPorcupine
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      カタログ番号 GTIN
      5.31091.0001 04055977242614