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500496 Porcn Inhibitor II, C59 - CAS 1243243-89-1 - Calbiochem

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Synonymes: 2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide, Wnt-C59, Wnt Pathway Inhibitor XVI

Primary Target: Porcupine (Porcn)-mediated Wnt palmitoylation
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500496
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Tableau de caractéristiques principal

CAS #Empirical Formula
1243243-89-1C₂₅H₂₁N₃O

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      Description
      OverviewA cell-permeable pyridinylphenyl-acetamide that is much more potent than IWP-2 (Cat. No. 681671) in inhibiting MBOAT family member Porcupine-mediated Wnt palmitoylation (IC50 = 74 pM in STF reporter assays using Wnt3a-transfected HEK293). Shown to be effective against Porcn of murine and human, but not xenopus, species and potently inhibit the processing of both canonical and non-canonical Wnt subtypes. C59 is demonstrated to be orally active and effectively suppress MMTV-WNT1 tumor expansion in mice (5 mg/kg & 10 mg/kg p.o.) in vivo.

      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 Number500496
      Brand Family Calbiochem®
      Synonyms2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide, Wnt-C59, Wnt Pathway Inhibitor XVI
      References
      ReferencesProffitt, K.D., et al. 2013. Cancer Res. 73, 502.
      Product Information
      CAS number1243243-89-1
      FormOff-white powder
      Hill FormulaC₂₅H₂₁N₃O
      Chemical formulaC₂₅H₂₁N₃O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPorcupine (Porcn)-mediated Wnt palmitoylation
      Purity≥99% 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 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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5004960002 04054839067495

      Documentation

      Porcn Inhibitor II, C59 - CAS 1243243-89-1 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Proffitt, K.D., et al. 2013. Cancer Res. 73, 502.
      Fiche technique

      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-September-2013 JSW
      Synonyms2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide, Wnt-C59, Wnt Pathway Inhibitor XVI
      DescriptionA cell-permeable pyridinylphenyl-acetamide that is much more potent than IWP-2 (Cat. No. 681671) in inhibiting MBOAT (membrane-bound O-acyltranferase) family member Porcn- (Porcupine) mediated Wnt palmitoylation (IC50 = 74 pM in STF reporter assays using Wnt3a-transfected HEK293 cells). Shown to be effective against Porcn of murine (mPorcn-A, B, C, D) and human (hPorcn-B), but not xenopus (xPorcn-A), species and potently inhibit the processing of both canonical (1, 2, 3a, 6, 7b, 8a, 9a, 9b, 10) and non-canonical (4, 5a, 11, 16) Wnt subtypes. C59 is orally active in mice (t1/2 = 1.94 h; plasma [C59]t = 24 h = 3 nM; 5 mg/mL p.o.) and demonstrated to effectively suppress MMTV-WNT1 tumor expansion in both immunodeficient female nude mice (Ave fold of tumor expansion = 3 vs.19 in 17 days with or without daily 10 mg/kg oral dosage) and in immunocompetent female nulliparous mice (Ave fold of tumor expansion = 0.8 vs.3.7 in 21 days with or without daily 5 mg/kg oral dosage) in vivo.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1243243-89-1
      Chemical formulaC₂₅H₂₁N₃O
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesProffitt, K.D., et al. 2013. Cancer Res. 73, 502.