LGK-974 (WNT-974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.
|Source||Nat Med (2015). Figure 5. LGK-974|
|Cell Lines||MCF-7 cells|
|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 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.|
|Incubation time||3 d|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 30 mg/mL|
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