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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1243243-89-1C₂₅H₂₁N₃O

Products

Catalog NumberPackaging Qty/Pack
5.00496.0001 Glass bottle 10 mg
5.00496.0002 Glass bottle
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
Catalog Number GTIN
5.00496.0001 04055977245615
5.00496.0002 04054839067495

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 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.