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NVP-LGK974 | Wnt inhibitor

  • NVP-LGK974 (.png)
Catalog #:

Product Description

LGK974 is a potent and orally active Wnt pathway inhibitor with an IC50<1 nM in the Wnt signaling assay [1]. It inhibits acylation of Wnt proteins by Porcupine (Porcn). LGK974 specifically blocks the proliferation of pancreatic cancer cells that have up-regulated Wnt signaling caused by carrying inactive mutations in a Ubiquitin E3 ligase, RNF43 [2].

LGK974 robustly suppressed Wnt signaling in vivo resulting in tumor regression in a murine breast cancer model driven by MMTV-Wnt1, and showed excellent efficacy in xenograft models of head and neck squamous cell carcinoma and pancreatic cancer [3]. Currently LGK974 is in the Phase I study to treat patients with different types of Wnt signaling-driven cancers [4].

Technical information:

Chemical Formula:   C23H20N6O
CAS #:   1243244-14-5
Molecular Weight:   396.44
Purity:   > 98%
Appearance:   White
Chemical Name:   2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   NVP-LGK974, LGK974

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


1. Shifeng Pan. Discovery of LGK974: A selective Porcupine inhibitor targeting Wnt signaling in cancer. AACR Annual Meeting 2013.
2. Jiang X, et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. Proc Natl Acad Sci USA. 2013; 110(31):12649-54. Pubmed ID: 23847203
3. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci U S A. 2013; 110(50):20224-9 Pubmed ID: 24277854
4. http://clinicaltrials.gov/show/NCT01351103

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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