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

A cell-permeable inhibitor of Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC₅₀ from 50 pM to 1.1 nM).

Porcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(2ʹ,3-Dimethyl-2,4ʹ-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974

Primary Target: Porcupine
531091
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
1243244-14-5C₂₃H₂₀N₆O

Products

KatalógusszámCsomagolás Menny./csomag
5.31091.0001 Üvegpalack 5 mg
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
Applications
Biological Information
Primary TargetPorcupine
Purity≥97% 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
Katalógusszám GTIN
5.31091.0001 04055977242614

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
Liu, J., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20224.
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.

Revision19-August-2014 JSW
Synonyms2-(2ʹ,3-Dimethyl-2,4ʹ-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974
DescriptionA cell-permeable C59 (Cat. No. 500496) structural analog that potently inhibits TM3 cellular Wnt pathway activation-dependent transcription by blocking Wnt secretion from co-cultured L-cells (IC50 from 50 pM to 1.1 nM using Wnt1/2/3/3a/6/7a/9a L-cell transfectants) via direct porcupine (Porcn), but not Wntless, affinity interaction. Shown to inhibit Wnt-dependent proliferation of head and neck squamous cell carcinoma (HNSCC) line HN30 (IC50 = 0.3 nM in 48 h colony formation assay), but not the growth of 293T even at concentrations as high as 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 harboring tumors derived from human HNSCC HN30 or tumor fragments from murine mammary tumor virus (MMTV)-Wnt1 transgenic mice, 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.
FormTan powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1243244-14-5
Chemical formulaC₂₃H₂₀N₆O
Purity≥97% by HPLC
SolubilityDMSO (50 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
ReferencesLiu, J., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20224.