化合物 LGK-974|T2618|TargetMol

LGK974
1243244-14-5

￥438 1mg 起订

￥632 2mg 起订

￥997 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 LGK-974

英文名称：: LGK974

CAS号：: 1243244-14-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥98%

产品类别：: 抑制剂

货号：: T2618

Product Introduction

Bioactivity

名称	LGK974
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.
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)
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].
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。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 73 mg/mL (184.1 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	WNT-974 \| WNT 974 \| Porcupine \| NVP-LGK-974 \| NVP-LGK 974 \| LGK974 \| Inhibitor \| inhibit
相关产品	ETC-159 \| Wnt-C59 \| IWP-2 \| WHN-88 \| IWP L6 \| GNF-6231 \| Porcn-IN-1 \| IWP-O1
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| ReFRAME 相关化合物库 \| 临床期小分子药物库 \| 口服活性化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 表型筛选靶点鉴定库 \| Wnt/Hedgehog/Notch 通路化合物库 \| 抗癌药物库

WNT974|||NVP-LGK974|||LGK-974|||LGK 974|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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