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GLPG0187

GLPG0187

产品编号 T4259   CAS 1320346-97-1

GLPG0187是整联蛋白受体的广谱拮抗剂,抑制αvβ1-integrin 的IC50值为1.3 nM,具有抗肿瘤活性。

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GLPG0187 Chemical Structure
GLPG0187, CAS 1320346-97-1
规格 价格/CNY 货期 数量
1 mg ¥ 995 现货
5 mg ¥ 2,730 现货
10 mg ¥ 3,730 现货
25 mg ¥ 5,950 现货
50 mg ¥ 8,380 现货
100 mg ¥ 11,300 现货
500 mg ¥ 22,600 现货
1 mL * 10 mM (in DMSO) ¥ 3,520 现货
产品目录号及名称: GLPG0187 (T4259)
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纯度: 100%
纯度: 99.12%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM).
靶点活性 αvβ1:1.3 nM
体外活性 GLPG0187 is an effective inhibitor of osteoclastic bone resorption and angiogenesis. In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors (IC50s: 1.3/3.7/2.0/1.4/1.2/7.7 nM, for αvβ1/3/5/6/8 and α5β1). GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio. GLPG0187 dose-dependently reduces the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells. GLPG0187 causes cell rounding and clumping. GLPG0187 dose-dependently and markedly reduces in tumor cell migration. At all concentrations, GLPG0187 markedly reduces cell proliferation.
体内活性 GLPG0187 obviously reduces their metastatic tumor growth by blocking αv-integrins. GLPG0187 markedly lows Bone tumor burden and markedly inhibits the number of bone metastases/mouse. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited by GLPG0187.
激酶实验 HSP90 competition isothermal calorimetry: Kd values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit
细胞实验 Tumour cell proliferation is determined using the MTS assay. PC3 cells are seeded at 10,000 cells/well in 96 well plates containing either GLPG0187 (0.5, 5, or 50 ng/mL), vehicle or media control, then cultured in 100 μL medium for 24 hr. Cell proliferation is analyzed using 20 μL MTS dye incubated for 3 hr at 37°C in the dark. Absorbance from each well (6/treatment) is quantified at 490 nm and the mean fluorescence calculated. The assay is repeated at 48, 72 and 96 hr, on three independent occasions.
动物实验 GLPG0187 is prepared in 1:1 dimethyl sulfoxide in PBS.The effect of GLPG0187 on bone loss is evaluated in 3-month-old castrated male mice after 4 weeks of treatment with dosing starting immediately after castration (preventive protocol). Two different modes of administration are used: either subcutaneous twice daily with 10, 30, or 100 mg/kg of GLPG0187, either oral, twice daily with 30, 100, or 300 mg/kg of GLPG0187.
分子量 595.71
分子式 C29H37N7O5S
CAS No. 1320346-97-1

存储

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

溶解度

DMSO: 5.96 mg/mL (10 mM)

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 1.6787 mL 8.3933 mL 16.7867 mL 41.9667 mL
5 mM 0.3357 mL 1.6787 mL 3.3573 mL 8.3933 mL
10 mM 0.1679 mL 0.8393 mL 1.6787 mL 4.1967 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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. van der Horst G, et al. Targeting of α(v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia. 2011 Jun;13(6):516-25. 2. Reeves KJ, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG20187. Int J Cancer. 2015 Apr 1;136(7):1731-40.
RGD peptide (GRGDNP) E7820 mP6 A-205804 Lifitegrast BT100 Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) β-glycosidase-IN-1

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 抗癌药物库 经典已知活性库 抑制剂库 口服活性化合物库 已知活性化合物库 药物功能重定位化合物库 细胞骨架化合物库 NO PAINS 化合物库

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
g
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
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% Tween 80
% ddH2O
计算 重置

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

GLPG0187 1320346-97-1 Cytoskeletal Signaling Integrin inhibit GLPG-0187 Inhibitor GLPG 0187 inhibitor

 

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