LGK974 CAS 1243244-14-5

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

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.

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

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366896 LGK974 (LGK-974, WNT-974, LGK 974, NVP-LGK974) CAS: 1243244-14-5

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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

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