LGK-974_Wnt beta-catenin_CAS号1243244-14-5说明书_AbMole中国

化学数据

分子量分子式CAS号储存条件

396.44C23H20N6O1243244-14-53年 -20°C 粉末状

溶解性（25°C）

DMSO 79 mg/mLWater <1 mg/mLEthanol <1 mg/mL

生物活性

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

实验操作 来自于公开的文献，仅供参考

细胞实验细胞系方法

HPAF-II, PaTu 8988S, and Capan-2 cells

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 μMLGK974. After 3 d, the cells are treated with fresh growth medium containing 20 μM EdU, which is included in the Click-iT EdU AlexaFluor 488 HCS assay kit, and the plate was incubated for 2 h at 37 °C in a humidified atmosphere containing 5% CO2. Cells are fixedwith final 4% (mass/vol) paraformaldehyde for 30 min, washed with PBS, permeabilized, and stained with 50 μg/mL Hoechst in PBSfor 30 min. After wash, the cells are proceeded to EdU detection according to the instruction of Click-iT EdU assay kit. Triplet wells areperformed for each condition.

浓度处理时间

~1 μM3 d

动物实验动物模型配制剂量给药处理

A murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30)10% (vol/vol) citrate buffer (pH 2.8)/90% (vol/vol) citrate buffer (pH 3.0) or 0.5% MC/0.5% Tween 80~3 mg/kg dailyOral gavage

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

小鼠

重量 (kg)体表面积 (m2)Km 系数

0.020.0073

动物 B的Km系数动物 A的Km系数

大鼠0.150.0256

兔1.80.1512

豚鼠0.40.058

仓鼠0.080.025

狗100.520

动物 A (mg/kg) = 动物 B (mg/kg) × 

例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

参考文献

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.