LGK974, Porcupine (Wnt) Inhibitor


Catalog No. size PriceQuantity
M60106-2D 10 mM DMSO (0.504 mL) $139
M60106-2S 2mg solid $139
M60106-10S 10mg solid $563

Description

Product information

CAS Number: 1243244-14-5

Molecular Weight: 396.44

Formula: C23H20N6O

Chemical Name: 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide

Smiles: CC1=CC(=CC=N1)C1=NC=C(CC(=O)NC2=CC=C(C=N2)C2=CN=CC=N2)C=C1C

InChiKey: XXYGTCZJJLTAGH-UHFFFAOYSA-N

InChi: InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 79 mg/mLwarmed(199.27 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

LGK974 effectively displaces [3H]-GNF-1331 with IC50 of 1 nM in the PORCN radioligand binding assay, and shows no major cytotoxicity in cells up to 20 µM. LGK974 shows comparable inhibitory activities against all tested Wnts with IC50 ranging from 0.05 to 2.4 nM, which is consistent with the genetic loss of PORCN phenotype. LGK974 specifically inhibits the growth of three RNF43-mutant cell lines, HPAF-II, PaTu 8988S, and Capan-2.

In Vivo:

In a murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30), LGK974 (3 mg/kg) inhibits Wnt signaling in vivo and induces tumor regression without significant body weight loss in the mice. LGK974 (5 mg/kg, p.o., BID) also inhibits tumor growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2) in vivo.

References:

  1. Jiang X, et al. Proc Natl Acad Sci U S A. 2013, 110(31), 12649-12654.
  2. Liu J, et al. Proc Natl Acad Sci U S A. 2013, 110(50), 20224-20229.

Products are for research use only. Not for human use.

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