化合物 Galunisertib|T2510

Galunisertib
700874-72-2

￥233 1mg 起订

￥329 2mg 起订

￥536 5mg 起订

上海更新日期：2024-09-15

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 化合物 Galunisertib

英文名称：: Galunisertib

CAS号：: 700874-72-2

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：: 99.98%

产品类别：: 抑制剂

货号：: T2510

Product Introduction

Bioactivity

名称	Galunisertib
描述	Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.
细胞实验	Cell survival was determined using the MTT assay. The conversion of yellow water-soluble tetrazolium MTT into purple insoluble formazan is catalyzed by mitochondrial dehydrogenases and used to estimate the number of viable cells. In brief, cells were seeded in 96-well tissue culture plates at a density of 2 × 103 cells/well. After drug exposure, cells were incubated with 0.4 mg/mL MTT for 4 hours at 37°C. After incubation, the supernatant was discarded, insoluble formazan precipitates were dissolved in 0.1 mL of DMSO, and the absorbance was measured at 560 nm by use of a microplate reader. Wells with untreated cells or with drug-containing medium without cells were used as positive and negative controls respectively. For proliferation assay, MTT assay was done daily to determine the number of viable cells in untreated control and galunisertib-treated group [2].
激酶实验	Briefly, the assay was first done at 30°C for 4 h in a 96-well plate containing 2 ng/mL TGF-bR KD, 100 mM Hepes pH 7.5, 4 mM MgCl2, 0.2 mM MnCl2, 0.4 mM sodium orthovanadate, 2 mM DL-dithiothreitol, and 10mM ATP. After incubation, 50mL of Kinase-Glo plus reagent was added and further incubated at 25°C for 30 min. Subsequently, a 100mL aliquot of each reaction mixture was transferred to a black mictotiter plate and the luminescence was measured by a vector counter. The inhibitory activity IC50 was tested in duplicate for each sample [1].
动物实验	Transgenic mice expressing a fusion gene (Alb/TGF) consisting of modified porcine TGF-β1 cDNA under the control of the regulatory elements of the mouse albumin gene (26) were used under animal institute approved protocol. Mice were given LY-2157299 at a dose of 100mg/kg/day in NaCMC/SLS/PVP/antifoam solution by gastric lavage using a curved 14 G needle. Blood counts were analyzed by the Advia machine. Mice femurs were flushed and bone marrows cells were used for clonogenic assays [3].
体外活性	方法: 小鼠胚胎成纤维细胞 NIH3T3 用 Berzosertib (0.0001-10 µM) 处理 2 h，随后用 TGFβ1 孵育过夜，使用 3H-thymidine proliferation assay 检测细胞增殖。结果: Berzosertib 抑制 TGFβ1 诱导的增殖，IC50 为 0.396 µM。[1] 方法: 七种 HCC 细胞系 JHH6、SK-HEP1、SK-Suni、SK-Sora、HepG2、Hep3B、HuH7 用 Galunisertib (1-10 µM) 和 TGF-β (5 ng/mL) 处理 5-24 h，使用 Western Blot 检测靶点蛋白表达水平。结果: 添加 Galunisertib 以剂量和时间依赖的方式降低了所有细胞系中 p-Smad2 的表达水平，与 TGF-β 诱导无关。[2]
体内活性	方法: 为检测体内抗肿瘤活性，用 Galunisertib (75 mg/kg，10% beta-cyclodextrin-HCl) 灌胃给药携带 MX1、Calu6 或 4T1 肿瘤的 athymic nu/nu 小鼠，每天两次，持续 20-40 天。结果: Galunisterib 单药治疗都导致了明显的肿瘤生长延迟。对于MX1，Galunisertib 治疗导致肿瘤生长延迟 10.3±4.3天。对于 Calu6，Galunisertib 治疗导致肿瘤生长推迟 8.3±2.6天。对于 4T1，Galunisertib 治疗导致肿瘤生长延迟 13±2.4天。[1]
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 : 50 mg/mL (135.35 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 6.9 mg/mL (18.68 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol : Insoluble
关键字	inhibit \| LY 2157299 \| Transforming growth factor beta receptors \| Inhibitor \| LY-2157299 \| TGF-β Receptor \| Galunisertib
相关产品	Monocrotaline \| Pirfenidone \| A 83-01 \| Halofuginone \| Chromenone 1 \| LY-364947 \| BMP signaling agonist sb4 \| SB-431542 \| Alantolactone \| LDN-193189 2HCl \| Hydrochlorothiazide \| Asiaticoside
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 \| 激酶抑制剂库 \| TGF-β/Smad靶点化合物库 \| 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 \| 抗癌药物库

LY2157299|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子