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Galunisertib

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产品编号 T2510Cas号 700874-72-2
别名 LY2157299

Galunisertib (LY2157299) 是一种 TGF-β 受体 I 型 (TGF-βRI) 抑制剂 (IC50=56 nM),具有选择性。Galunisertib 具有抗肿瘤活性,可与 PD-1 抑制剂联合治疗。

Galunisertib

Galunisertib

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纯度: 100%
产品编号 T2510 别名 LY2157299Cas号 700874-72-2

Galunisertib (LY2157299) 是一种 TGF-β 受体 I 型 (TGF-βRI) 抑制剂 (IC50=56 nM),具有选择性。Galunisertib 具有抗肿瘤活性,可与 PD-1 抑制剂联合治疗。

规格价格库存数量
1 mg¥ 233现货
2 mg¥ 329现货
5 mg¥ 536现货
10 mg¥ 812现货
25 mg¥ 1,480现货
50 mg¥ 2,580现货
100 mg¥ 3,590现货
200 mg¥ 5,190现货
500 mg¥ 8,090现货
1 g¥ 10,900现货
1 mL x 10 mM (in DMSO)¥ 498现货
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产品介绍

生物活性
产品描述
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.
靶点活性
TβRI:56 nM (cell free)
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]
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].
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].
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].
别名LY2157299
化学信息
分子量369.42
分子式C22H19N5O
CAS No.700874-72-2
SmilesCc1cccc(n1)-c1nn2CCCc2c1-c1ccnc2ccc(cc12)C(N)=O
密度1.40 g/cm3
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: 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
溶液配制表
1mg5mg10mg50mg
1 mM2.7069 mL13.5347 mL27.0695 mL135.3473 mL
5 mM0.5414 mL2.7069 mL5.4139 mL27.0695 mL
10 mM0.2707 mL1.3535 mL2.7069 mL13.5347 mL
1mg5mg10mg50mg
20 mM0.1353 mL0.6767 mL1.3535 mL6.7674 mL
50 mM0.0541 mL0.2707 mL0.5414 mL2.7069 mL
100 mM0.0271 mL0.1353 mL0.2707 mL1.3535 mL

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
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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

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