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

500496
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₅H₂₁N₃O 1243243-89-1

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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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Proffitt, K.D., et al. 2013. Cancer Res. 73, 502.
          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-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 +2°C to +8°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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesProffitt, K.D., et al. 2013. Cancer Res. 73, 502.