Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 69 mg/mL (186.8 mM)
Ethanol: Insoluble
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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