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GNF-6231

Names

[ CAS No. ]:
1243245-18-2

[ Name ]:
GNF-6231

[Synonym ]:
N-[5-(4-Acetyl-1-piperazinyl)-2-pyridinyl]-2-(2'-fluoro-3-methyl-2,4'-bipyridin-5-yl)acetamide
[2,4'-Bipyridine]-5-acetamide, N-[5-(4-acetyl-1-piperazinyl)-2-pyridinyl]-2'-fluoro-3-methyl-

Biological Activity

[Description]:

GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.1) GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested2) GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration.3) The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg.4) GNF-6231 showed very robust dose-related antitumor efficacy.

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> Porcupine
Research Areas >> Cancer

[References]

[1]. Cheng D et al. Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors. ACS Med Chem Lett. 2016 May 10;7(7):676-80.


[Related Small Molecules]

LGK-974 (WNT974) | Wnt-C59 | IWP L6 | Porcupine-IN-1

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
746.0±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H25FN6O2

[ Molecular Weight ]:
448.493

[ Flash Point ]:
405.0±32.9 °C

[ Exact Mass ]:
448.202301

[ LogP ]:
0.79

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.627

[ Storage condition ]:
-20℃

Related Compounds