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LGK-974 (WNT-974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.
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Source | Nat Med (2015). Figure 5. LGK-974 |
| Method | Western blot | |
| Cell Lines | MCF-7 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 48 h | |
| Results | LGK-974 (1 μM), an inhibitor of Wnt ligands, decreased fentanyl-activated b-catenin, p-GSK-3b (Ser9) and FUT8 expression |
| 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 |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Molecular Weight | 396.44 |
| Formula | C23H20N6O |
| CAS Number | 1243244-14-5 |
| Purity | 99.29% |
| Solubility | DMSO 30 mg/mL |
| Storage | at -20°C |
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