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GSK2256098

GSK2256098

产品编号 T2281   CAS 1224887-10-8
别名: GSK 2256098, GSK-2256098, GTPL7939

GSK2256098 (GTPL7939) 是一种选择性FAK 激酶抑制剂,抑制胰腺癌细胞的生长和存活。

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GSK2256098 Chemical Structure
GSK2256098, CAS 1224887-10-8
规格 价格/CNY 货期 数量
1 mg ¥ 322 现货
2 mg ¥ 463 现货
5 mg ¥ 728 现货
10 mg ¥ 1,130 现货
25 mg ¥ 2,260 现货
50 mg ¥ 3,480 现货
100 mg ¥ 4,900 现货
500 mg ¥ 9,870 现货
1 mL * 10 mM (in DMSO) ¥ 786 现货
其他形式的 GSK2256098:
产品目录号及名称: GSK2256098 (T2281)
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选择批次  
纯度: 99.52%
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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 GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.
靶点活性 FAK:0.4 nM(Ki)
体外活性 GSK2256098 has been developed to inhibit FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397. After a 30-min incubation, GSK2256098 inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87 mg (brain), and A549 (lung), at IC50 values of 15, 8.5 and 12 nM, respectively. In addition, the data suggests that cellular inhibition of FAK by GSK2256098 can occur as early as 30 min in cultured cells and lasts up to 12 hours in mouse tumor xenografts. GSK2256098 inhibition of FAK kinase activity can decrease Akt and ERK activity. PI3K/Akt and ERK signaling contributes to cell survival, implying a pharmacological value of GSK2256098 in attenuation of abnormal survival pathways in specific types of PDAC cells. GSK2256098 can promote apoptosis in L3.6P1 cells through caspase-9/PARP-related pathways. It attenuates abnormal growth and aberrant motility of PDAC cells in a FAK specific manner[1]. GSK2256098 also inhibits growth, migration, and invasion and induces apoptosis in a subset of GBM cell lines[2].
体内活性 Pharmacokinetic (PK) studies in mice and rats with an intact blood brain barrier indicate that the penetration of GSK2256098 into the CNS is poor. However, it achieves concentrations in tumor of patients with GBM(glioblastoma) exceeding those associated with preClinicalal activity[2]. GSK2256098 has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD (maximum tolerated dose), and has Clinicalal activity in patients with mesothelioma, particularly those with merlin loss[3]. In the Ishikawa orthoptopic murine model, treatment with GSK2256098 results in lower tumor weights and fewer metastases than mice inoculated with Hec1A cells. Tumors treated with GSK2256098 have lower microvessel density (CD31), less cellular proliferation (Ki67), and higher apoptosis (TUNEL) rates in the Ishikawa model when compared to the Hec1a model. GSK2256098 may be therapeutically beneficial to patients with PTEN-mutant uterine cancer, and PTEN represents a potential predictive biomarker[4].
细胞实验 PDAC cells are cultured on a 6-well plate. When cell confluence reachs about 70% in regular medium, the cells are incubated in the medium containing 0.1-10 μM GSK2256098 for 48 or 72 hr. At the end of treatments, cells are re-seeded and kept for 9 d Then, the cells are stained using Clonogenic Reagent, and the blue colonies are counted. (Only for Reference)
别名 GSK 2256098, GSK-2256098, GTPL7939
分子量 414.89
分子式 C20H23ClN6O2
CAS No. 1224887-10-8

存储

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

溶解度

DMSO: 76 mg/mL (183.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 76 mg/mL (183.2 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 / Ethanol 1 mM 2.4103 mL 12.0514 mL 24.1028 mL 60.2569 mL
5 mM 0.4821 mL 2.4103 mL 4.8206 mL 12.0514 mL
10 mM 0.241 mL 1.2051 mL 2.4103 mL 6.0257 mL
20 mM 0.1205 mL 0.6026 mL 1.2051 mL 3.0128 mL
50 mM 0.0482 mL 0.241 mL 0.4821 mL 1.2051 mL
100 mM 0.0241 mL 0.1205 mL 0.241 mL 0.6026 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. Zhang J, et al. Cell Cycle. 2014, 13(19):3143-9. 2. Paul Mulholland, et al. Neuro Oncol. 2015, 17(Suppl 5): v11. 3. Soria JC, et al. Ann Oncol. 2016, 27(12):2268-2274. 4. Thanapprapasr D, et al. Mol Cancer Ther. 2015, 14(6):1466-75. 5. Auger KR, et al. Eur J Cancer. 2012, 48:118

文献引用

1. Zhang P, Cao X, Guan M, et al. CPNE8 Promotes Gastric Cancer Metastasis by Modulating Focal Adhesion Pathway and Tumor Microenvironment. International Journal of Biological Sciences. 2022, 18(13): 4932-4949.
Karanjin Antimycin A2c Y-27632 Hydroxy-PP-Me ONC212 LYG-202 (+)-Nortrachelogenin Pictilisib

相关化合物库

该产品包含在如下化合物库中:
细胞凋亡化合物库 抗癌化合物库 表型筛选靶点鉴定库 药物功能重定位化合物库 酪氨酸激酶分子库 激酶抑制剂库 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
%
% 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

GSK2256098 1224887-10-8 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK Focal adhesion kinase PTK2 protein tyrosine kinase 2 GTPL 7939 GSK 2256098 Inhibitor GSK-2256098 GTPL-7939 GTPL7939 inhibit PTK2 inhibitor

 

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