1243245-18-2

Usage

Uses

Used in Pharmaceutical Industry:
N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2’-fluoro-3-methyl-2,4’-bipyridin-5-yl)acetamide is used as a Wnt signaling modulator for the development of targeted cancer therapies. The blockade of aberrant Wnt signaling, which is often implicated in the progression of various cancers, makes N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2’-fluoro-3-methyl-2,4’-bipyridin-5-yl)acetamide an attractive therapeutic approach. By modulating the Wnt signaling pathways, GNF-6231 has the potential to inhibit tumor growth and reduce the risk of metastasis in cancer patients.

Upstream product

• 959795-77-8 1-(4-(6-aminopyridin-3-yl)piperazin-1-yl)ethan-1-one 
• 1243246-17-4 2-(2'-fluoro-3-methyl-2,4'-bipyridin-5-yl)acetic acid 
• 29241-60-9 5-bromo-2-chloro-3-methylpyridine 
• 1243245-77-3 tert-butyl 2-(6-chloro-5-methylpyridin-3-yl)acetate 

Relevant academic research and scientific papers

Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors

Blockade of aberrant Wnt signaling is an attractive therapeutic approach in multiple cancers. We developed and performed a cellular high-throughput screen for inhibitors of Wnt secretion and pathway activation. A lead structure (GNF-1331) was identified from the screen. Further studies identified the molecular target of GNF-1331 as Porcupine, a membrane bound O-acyl transferase. Structure-activity relationship studies led to the discovery of a novel series of potent and selective Porcupine inhibitors. Compound 19, GNF-6231, demonstrated excellent pathway inhibition and induced robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model.

N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS

The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.