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GSK2256098

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Chemical Structure| 1224887-10-8 同义名 : GTPL7939
CAS号 : 1224887-10-8
货号 : A318281
分子式 : C20H23ClN6O2
纯度 : 99%+
分子量 : 414.889
MDL号 : MFCD30502650
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(72.31 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • FAK

    FAK, Ki:0.4 nM
描述 FAK (Focal adhesion kinase), a non-receptor tyrosine kinase, can regulate the cytoskeleton and act as a scaffolding and signaling protein for other adhesion molecules. The expression of FAK and its phosphorylation status show a strong correlation with the invasive phenotype of aggressive human tumors. GSK2256098 is a selective FAK inhibitor with Ki value of 0.4nM. Cellular study showed that GSK2256098 inhibited p-FAK with IC50 values ranging in 2-15nM while only showed effective on cell growth inhibition in cell lines in anchorage-independent conditions with soft agar or methylcellulose, but not in standard conditions on tissue culture plastic in tested[1]. Another study showed that GSK2256098 could dose-dependently inhibit FAK activity on its phosphorylation site with different potency according to different PDAC cells, most potent to L3.6P1 and least potent to PANC-1 cells, at concentration ranging in 0.1-10μM, as well as promote apoptosis in L3.6P1 cells through caspase-9/PARP, but showed inhibition of cell growth only in anchorage-independent manner. In vitro wound healing assays showed that pre-treatment with GSK2256098 at concentration ranging in 1-25μM for 48h caused impairment of cell motility dose-dependently in L3.6P1 and PANC-1 cells[2]. Oral administration of GSK2256098 caused dose-dependent reduction of pFAK with maximal reduction corresponding to the Cmax of GSK2256098 in mice bearing subcutaneous human tumors, suggesting the good pharmacodynamics of GSK2256098[1].
作用机制 GSK2256098 is an ATP competitive inhibitor which can bound in the ATP binding pocket of FAK.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.05mL

2.41mL

1.21mL

24.10mL

4.82mL

2.41mL
参考文献

[1]Zhang J, He DH, et al. A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells. Cell Cycle. 2014;13(19):3143-9.