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Galunisertib

Galunisertib

产品编号 T2510   CAS 700874-72-2
别名: LY2157299

Galunisertib (LY2157299) 是一种TGF-β 受体 I 型 (TGF-βRI) 激酶的选择性抑制剂,其IC50=56 nM。

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Galunisertib Chemical Structure
Galunisertib, CAS 700874-72-2
规格 价格/CNY 货期 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 * 10 mM (in DMSO) ¥ 498 现货
其他形式的 Galunisertib:
产品目录号及名称: Galunisertib (T2510)
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选择批次  
纯度: 100%
纯度: 99.98%
纯度: 99.85%
纯度: 97.09%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Galunisertib (LY2157299) is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
靶点活性 TβRI:56 nM (cell free)
体外活性 The HCC cell lines were simultaneously exposed to 0.1, 1, 10, and 100 μM galunisertib (LY-2157299) with 5 μM sorafenib in presence of TGF-β for 72 hours. Galunisertib displayed a slight dose-dependent potentiation of sorafenib in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines [2]. Leukemic cells (K562) and marrow stromal cells (HS-5) were treated with TGF-β1 (20 ng/ml) in the presence and absence of LY-2157299 (5 μM) and assessed for SMAD2 phosphorylation by immunoblotting. LY-2157299 pretreatment (1 hr) led to attenuation of activation/phosphorylation of SMAD2 [3].
体内活性 Mice transgenic for alb/TGF-β were treated with either LY-2157299 (100 mg/kg/d) or vehicle daily by gastric lavage for 14 days. Blood counts were done on the 14th day and revealed a significant rise in hematocrit after LY-2157299 treatment. The mice were sacrificed and bone marrow biopsies were immunostained with an antibody against phosphor-SMAD2. Representative sample shows inhibition of SMAD2 activation after LY-2157299 treatment [3]. After oral administration of 75 mg/kg, LY2157299 induced a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline was approximately 6 h after administration [4].
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
分子量 369.42
分子式 C22H19N5O
CAS No. 700874-72-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 69 mg/mL (186.8 mM)

Ethanol: Insoluble

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7069 mL 13.5347 mL 27.0695 mL 67.6737 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 mL 13.5347 mL
10 mM 0.2707 mL 1.3535 mL 2.7069 mL 6.7674 mL
20 mM 0.1353 mL 0.6767 mL 1.3535 mL 3.3837 mL
50 mM 0.0541 mL 0.2707 mL 0.5414 mL 1.3535 mL
100 mM 0.0271 mL 0.1353 mL 0.2707 mL 0.6767 mL

计算器

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参考文献

1. Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim). 2014 Sep;347(9):609-15. 2. Serova M, et al. Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6(25):21614-27. 3. Zhou L, et al. Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase. Cancer Res. 2011 Feb 1;71(3):955-63. 4. Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. 5. Li W, Tibben M, Wang Y, et al. P‐glycoprotein (MDR1/ABCB1) controls brain accumulation and intestinal disposition of the novel TGF‐β signaling pathway inhibitor galunisertib[J]. International journal of cancer. 2020, 146(6): 1631-1642 6. Lu H H, Lin S Y, Weng R R, et al. Fucosyltransferase 4 shapes oncogenic glycoproteome to drive metastasis of lung adenocarcinoma[J]. EBioMedicine. 2020, 57: 102846 7. Mei Y, Jiang T, Zou Y, et al. Fucosyltransferase 4 shapes oncogenic glycoproteome to drive metastasis of lung adenocarcinoma[J]. EBioMedicine. 2020, 57: 102846. 8. Su Q, Fan M, Wang J, et al. Sanguinarine inhibits epithelial–mesenchymal transition via targeting HIF-1α/TGF-β feed-forward loop in hepatocellular carcinoma[J]. Cell Death & Disease. 2019, 10(12): 1-15.

文献引用

1. Su Q, Fan M, Wang J, et al. Sanguinarine inhibits epithelial–mesenchymal transition via targeting HIF-1α/TGF-β feed-forward loop in hepatocellular carcinoma. Cell Death & Disease. 2019, 10(12): 1-15 2. Lu H H, Lin S Y, Roc Weng R, et al. Fucosyltransferase 4 shapes oncogenic glycoproteome to drive metastasis of lung adenocarcinoma. EBioMedicine. 2020, 57: 102846 3. Zhu M, Tang X, Gong Z, et al. TAD1822-7 induces ROS-mediated apoptosis of HER2 positive breast cancer by decreasing E-cadherin in an EphB4 dependent manner. Life Sciences. 2021: 119954 4. Li W, Tibben M, Wang Y, et al. P‐glycoprotein (MDR1/ABCB1) controls brain accumulation and intestinal disposition of the novel TGF‐β signaling pathway inhibitor galunisertib. International Journal of Cancer. 2020, 146(6): 1631-1642 5. Windhaber C, Heckl A, Csukovich G, et al.A matter of differentiation: equine enteroids as a model for the in vivo intestinal epithelium.Veterinary Research.2024, 55(1): 1-21.
Nisevokitug PF-06952229 SJ000291942 Hesperetin Myristoyl tetrapeptide-12 Halofuginone hydrobromide ML347 SB-431542

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 TGF-β/Smad靶点化合物库 抗癌活性化合物库 抗癌临床化合物库 抗乳腺癌化合物库 干细胞分化化合物库 抗纤维化化合物库 抗肝癌化合物库 表型筛选靶点鉴定库 血液病分子库

剂量换算

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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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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g
给药体积
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第二步: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。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Galunisertib 700874-72-2 Stem Cells TGF-beta/Smad inhibit LY 2157299 LY2157299 Transforming growth factor beta receptors Inhibitor LY-2157299 TGF-β Receptor inhibitor

 

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