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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      5.00496.0001
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          Glass bottle 10 mg
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          5.00496.0002
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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®
              SynonymsWnt-C59, Wnt Pathway Inhibitor XVI, 2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide
              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
              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

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