Technical Data

366896
CAS Number
1243244-14-5
Grade
Highly Purified
Molecular Formula
C₂₃H₂₀N₆O
Molecular Weight
396.44
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
4°C
LGK974 (LGK-974, WNT-974, LGK 974, NVP-LGK974)
2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide; LGK-974; WNT-974; LGK 974; NVP-LGK974; 2’,3-Dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4’-bipyridine]-5-acetamide; 2-(2’,3-Dimethyl-[2,4’-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide

LGK974 is a highly potent inhibitor of Porcupine (PORCN), a Wnt-specific acyltransferase. LGK974 is orally bioavailable and inhibits WNT signaling in vitro and in vivo. It is reported to exhibit anti-tumor properties without increasing cytotoxicity

Synonyms
2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide; LGK-974; WNT-974; LGK 974; NVP-LGK974; 2’,3-Dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4’-bipyridine]-5-acetamide; 2-(2’,3-Dimethyl-[2,4’-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
CAS Number
1243244-14-5
Molecular Formula
C₂₃H₂₀N₆O
Molecular Weight
396.44
Purity (HPLC)
≥95%
Appearance
Off-white to white solid
Melting Point
176-180°C (lit)
Solubility
Chloroform (Slightly), Methanol (Slightly)
Method for Determining Identity
Proton NMR Spectroscopic and Mass Spectrometric analysis
TLC Conditions
SiO2; Dichloromethane: Methanol=9:1; Visualized with UV and AMCS; Single Spot, Rf=0.40
Water Content (KF)
As Reported
Storage and Stability
May be stored at RT for short-term only. Long-term storage is recommended at 4ºC for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.

References
1. Liu, J., Pan, S., Hsieh, M. H., Ng, N., Sun, F., Wang, T., Li, J. (2013). Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proceedings of the National Academy of Sciences,110(50), 20224-20229. 2. Glackin, C. A. (2014). Targeting the Twist and Wnt signaling pathways in metastatic breast cancer. Maturitas, 79(1), 48-51. 3. Pan, S., Cheng, D., Liu, J., Zhang, G., Hsieh, M. H., Ng, N., Harris, J. L. (2014, August). Discovery of LGK974, a potent and selective Porcupine inhibitor targeting Wnt signaling. In ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY (Vol. 248). 1155 16TH ST, NW, WASHINGTON, DC 20036 USA: AMER C SOC.
USBio References
No references available
United States Biological | 4 Technology Way | Salem, MA 01970
Phone 800-520-3011 | Fax 978-594-8052 | Website www.usbio.net