A potent, bioavailable inhibitor of PORCN
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LGK974

Item No. 14072

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2',3-dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4'-bipyridine]-5-acetamide
CAS Number
1243244-14-5
Synonyms
  • PORCN Inhibitor IV
Molecular Formula
C23H20N6O
Formula Weight
396.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
210, 300 nm
SMILES
CC1=CC(C2=NC=C(CC(NC3=CC=C(C4=CN=CC=N4)C=N3)=O)C=C2C)=CC=N1
InChi Code
InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
InChi Key
XXYGTCZJJLTAGH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $41

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    1 mg

    $75

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    5 mg

    $215

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    Cayman Chemical
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    Product Description

    LGK974 is a potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM).1 It greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity.1 LGK974 is orally bioavailable in mice and induces tumor regression in mouse breast tumors produced by mammary tumor virus-driven Wnt1 signaling.1 It also blocks carcinogenesis in other Wnt-related tumors at doses that have limited impact on stem cell renewal.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, J., Pan, S., Hsieh, M.H., et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc. Natl. Acad. Sci. USA 110(50), 20224-20229 (2013).

    2. Jiang, X., Hao, H.X., Growney, J.D., et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. Proc. Natl. Acad. Sci. USA 110(31), 12649-12654 (2013).

    3. Lum, L., and Clevers, H. The unusual case of porcupine. Science 337, 922-923 (2012).