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LY2109761

产品编号 T2123 CAS 700874-71-1

LY2109761 是一种新型选择性 TGF-β 受体 I/II 型 (TβRI/II) 双重抑制剂，Ki 分别为 38 nM 和 300 nM。

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LY2109761, CAS 700874-71-1

规格	价格/CNY	货期
1 mg	￥ 251	现货
2 mg	￥ 367	现货
5 mg	￥ 663	现货
10 mg	￥ 1,160	现货
25 mg	￥ 2,130	现货
50 mg	￥ 3,570	现货
100 mg	￥ 5,230	现货
200 mg	￥ 7,390	现货
1 mL * 10 mM (in DMSO)	￥ 728	现货

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纯度: 99.83%

纯度: 99.64%

纯度: 97%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.
靶点活性	TβRI:38 nM (Ki, cell free), TβRII:300 nM (Ki, cell free)
体外活性	Targeting TβRI/II kinase activity with LY2109761 (5 μM) almost completely suppressed both the basal (P = 0.0107) and TGF-β1–stimulated migration of L3.6pl/GLT cells (P < 0.0001), indicating that the migration of L3.6pl/GLT cells in vitro is effectively driven by endogenous TGF-β [1]. LY2109761 (0.001-0.1 μM) up-regulates (P < 0.001) E-cadherin mRNA and protein levels. This increase was localized at the cellular membrane where E-cadherin mediates anchorage that is cell-cell dependent [2]. LY2109761 (10 μM) or radiation (4 Gy) alone reduced neurosphere-forming efficiency in NMA-23 cells. The combination of LY2109761 plus radiation had supra-additive effects in neurosphere formation and limiting dilution assays [3].
体内活性	LY2109761 (50 mg/kg, p.o.) greatly reduced the tumor volume and increased the median survival duration of the mice to 45.0 days, but the differences were not significant. Only when LY2109761 was combined with gemcitabine were significant effects noted on tumor volume (P < 0.05) and median survival duration, which was increased to 77.5 days (P = 0.0018) [1]. In an orthotopic intracranial model, LY2109761 significantly reduced tumor growth, prolonged survival, and extended the prolongation of survival induced by radiation treatment. Histologic analyses showed that LY2109761 inhibited tumor invasion promoted by radiation, reduced tumor microvessel density, and attenuated mesenchymal transition [3].
细胞实验	LY2109761 cytotoxicity was determined by 3 methods: the MTT assay, manual counting of viable cells, and propidium iodide staining. MTT yields a purple formazan product that is detected using a 96-well plate reader at 570 nm. Cells were plated and cultured for 2 days in a 1% fetal bovine serum medium supplemented with LY2109761 at the following concentrations: 0.001, 0.01, 0.1, 1, 10, and 20 μM. Each experimental condition was reproduced in 8 wells, and each experiment was repeated 3 times. To confirm the cytotoxic data, cells were incubated under the described conditions and stained with the vital dye trypan blue, which does not react with the cell membrane because of its negative charge. All the unstained cells were counted using a hemocytometer. Four squares were counted for each condition, and each condition was repeated in triplicate in the same experiment. Each experiment was repeated 3 times for each cell line. Bars represent the average and standard deviation of all experiments. Under the same experimental conditions, nonpermeabilized cells were stained with propidium iodide and analyzed with a flow cytometer [2].
动物实验	Three days after the orthotopic implantation of 1.0 × 106 L3.6pl/GLT tumor cells in 50 μL of HBSS, when bioluminescence imaging confirmed that tumors were well established, 40 mice were randomly allocated into four groups (n = 10 mice per group) to receive one of the following treatments. (a) Vehicle solution for 50 μL of LY2109761 twice a day p.o. (days 1–5 of each week) and 50 μL of sterile saline daily i.p. (days 2 and 5 of each week; control group). (b) LY2109761 (50 mg/kg) twice a day p.o. (days 1–5 of each week) and 50 μL of sterile saline daily i.p. (days 2 and 5 of each week). (c) Gemcitabine (25 mg/kg) daily i.p. (days 2 and 5 of each week) and p.o. vehicle for 50μL of LY2109761 twice a day (days 1–5 of each week). (d) LY2109761 (50 mg/kg) twice a day (days 1–5 of each week) and gemcitabine (25 mg/kg) daily i.p. (days 2 and 5 of each week). Treatments were continued for 4 wk. All mice were weighed weekly and observed for tumor growth. Tumor diameter was assessed with a Vernier caliper, and tumor volume (mm3) was calculated as d2 × D/2, wherein d and D represent the shortest and longest diameters, respectively. Bulky disease was considered present when the tumor burden was prominent in the mouse abdomen (tumor volume, ≥2,000 mm3). When at least 6 of 10 mice in a treatment group presented with bulky disease, the median survival duration for that group was considered to be reached. At the median survival duration of the control group, the tumor growth in mice in all groups was evaluated using the bioluminescence emitted by the tumor cells. Bioluminescence imaging was conducted using a cryogenically cooled IVIS 100 imaging system coupled to a data acquisition computer running Living Image software. The mice were sacrificed by carbon dioxide inhalation when evidence of advanced bulky disease was present. The day of sacrifice was considered the day of death for survival evaluation [1].

分子量	441.52
分子式	C26H27N5O2
CAS No.	700874-71-1

存储

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

溶解度

DMSO: 6.88 mg/mL (15.57 mM)

Ethanol: Insoluble

H2O: 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	2.2649 mL	11.3245 mL	22.649 mL	56.6226 mL
	5 mM	0.453 mL	2.2649 mL	4.5298 mL	11.3245 mL
	10 mM	0.2265 mL	1.1325 mL	2.2649 mL	5.6623 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Melisi D, et al. LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol Cancer Ther. 2008 Apr;7(4):829-40. 2. Fransvea E, et al. Blocking transforming growth factor-beta up-regulates E-cadherin and reduces migration and invasion of hepatocellular carcinoma cells.Hepatology. 2008 May;47(5):1557-66. 3. Zhang M, et al. Blockade of TGF-β signaling by the TGFβR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res. 2011 Dec 1;71(23):7155-67.

文献引用

1. Huang X, Han L, Wang R, et al. Dual-responsive nanosystem based on TGF-β blockade and immunogenic chemotherapy for effective chemoimmunotherapy. Drug Delivery. 2022, 29(1): 1358-1369 2. Lu Z Z, Sun C, Zhang X, et al.Neuropilin 1 is an entry receptor for KSHV infection of mesenchymal stem cell through TGFBR1/2-mediated macropinocytosis.Science Advances.2023, 9(21): eadg1778. 3. Han L, Huang X, Zhao B, et al.TGF-β1 mediates tumor immunosuppression aggravating at the late stage post-high-light-dose photodynamic therapy.Cancer Immunology, Immunotherapy.2023: 1-17.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

LY2109761 700874-71-1 Autophagy Stem Cells TGF-beta/Smad TGF-β Receptor Transforming growth factor beta receptors Inhibitor inhibit LY 2109761 LY-2109761 inhibitor

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LY2109761

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

技术支持

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