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LGK974

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产品编号 T2618Cas号 1243244-14-5
别名 WNT974, NVP-LGK974, LGK-974, LGK 974

LGK974 (NVP-LGK974) 是一种有效的、特异性的、具有口服活性的Porcupine(PORCN) 抑制剂(IC50:0.1 nM)。

LGK974
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LGK974

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纯度: 100%
产品编号 T2618 别名 WNT974, NVP-LGK974, LGK-974, LGK 974Cas号 1243244-14-5

LGK974 (NVP-LGK974) 是一种有效的、特异性的、具有口服活性的Porcupine(PORCN) 抑制剂(IC50:0.1 nM)。

规格价格库存数量
1 mg
¥ 438
现货
2 mg
¥ 632
现货
5 mg
¥ 997
现货
10 mg
¥ 1,790
现货
25 mg
¥ 3,210
现货
50 mg
¥ 4,680
现货
100 mg
¥ 6,680
现货
1 mL x 10 mM (in DMSO)
¥ 941
现货
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TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
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产品介绍

生物活性
产品描述
LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
靶点活性
Porcn:0.4 nM
体外活性
在小鼠MMTV-WNT1肿瘤模型和人的头、颈部鳞状细胞癌模型(hn30)中,LGK-974(3 mg/kg)对Wnt信号通路有抑制作用,其可诱导肿瘤退化且不影响小鼠体重.LGK-974(5 mg/kg,2次/天,p.o.)还可抑制RNF43-突变胰腺肿瘤(HPAF-II 和Capan-2)的生长
体内活性
LGK-974对测试的Wnts均有抑制作用(IC50:0.05-2.4 nM)。 在PORCN放射配体结合测定中,LGK-974可有效取代[3H]GNF -1331(IC50:1 nM),且20 μM时细胞毒性也较小。LGK-974可特异抑制RNF43突变细胞株HPAF-II、PaTu 8988S和 Capan-2的生长。
激酶实验
Radioligand binding assay: using the aforementioned membrane preps, filtration binding assays are performed. To reduce nonspecific binding, 96-well filtration plates are precoated as suggested by the manufacturer with 0.1% BSA and then washed four times with 0.1% BSA. Membrane preps (50 μg total protein) are incubated in polypropylene 96-well plates with 6.6 nM 3H-GNF-1331 in the presence or absence of a testing compound in binding buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 0.1% BSA) plus EDTA-free protease inhibitor mixture in a final volume of 150 μL for 3 h at room temperature. Binding reaction mixtures are then transferred to the precoated 96-well filtration plates, filtered, and washed using a 96-pin FilterMate Harvester. Radioactive signals are obtained using a Microplate Scintillation Counter TopCount. Curve fitting is performed using Prism[1].
细胞实验
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 humidi?ed atmosphere containing 5% CO2. Cells are ?xed with ?nal 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. (Only for Reference)
别名WNT974, NVP-LGK974, LGK-974, LGK 974
化学信息
分子量396.44
分子式C23H20N6O
CAS No.1243244-14-5
SmilesCc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
密度1.268 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 73 mg/mL (184.14 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.5224 mL12.6122 mL25.2245 mL126.1225 mL
5 mM0.5045 mL2.5224 mL5.0449 mL25.2245 mL
10 mM0.2522 mL1.2612 mL2.5224 mL12.6122 mL
20 mM0.1261 mL0.6306 mL1.2612 mL6.3061 mL
50 mM0.0504 mL0.2522 mL0.5045 mL2.5224 mL
100 mM0.0252 mL0.1261 mL0.2522 mL1.2612 mL

SCI 文献

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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