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LGK-974

Cat. No. M2812
LGK-974 Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 220 In stock
50mg USD 640 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.

Protocol
Cell Experiment
Cell lines HPAF-II, PaTu 8988S, and Capan-2 cells
Preparation method Cells are plated in growth medium in a 96-well plate at a density of 6,000–12,000 cells per well and treated with DMSO or 1 μM LGK974. After 3 d, the cells are treated with fresh growth medium containing 20 μM EdU, which is included in the Click-iT EdU Alexa Fluor 488 HCS assay kit, and the plate was incubated for 2 h at 37 °C in a humidified atmosphere containing 5% CO2. Cells are fixed with final 4% (mass/vol) paraformaldehyde for 30 min, washed with PBS, permeabilized, and stained with 50 μg/mL Hoechst in PBS for 30 min. After wash, the cells are proceeded to EdU detection according to the instruction of Click-iT EdU assay kit. Triplet wells are performed for each condition.
Concentrations ~1 μM
Incubation time 3 d
Animal Experiment
Animal models A murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30)
Formulation 10% (vol/vol) citrate buffer (pH 2.8)/90% (vol/vol) citrate buffer (pH 3.0) or 0.5% MC/0.5% Tween 80
Dosages ~3 mg/kg daily
Administration Oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 396.44
Formula C23H20N6O
CAS Number 1243244-14-5
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

Differentiation of mesenchymal stem cells into cardiomyocytes is regulated by miRNA-1-2 via WNT signaling pathway.
Shen X, et al. J Biomed Sci. 2017 May 10;24(1):29. PMID: 28490365.

Wnt inhibition induces persistent increases in intrinsic stiffness of human trabecular meshwork cells.
Morgan JT, et al. Exp Eye Res. 2015 Mar;132:174-8. PMID: 25639201.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LGK-974 supplier, Wnt/beta-catenin, inhibitors

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