产品
编 号：F687647
分子式：C20H21N3O2S
分子量：367.46
分子式：C20H21N3O2S
分子量：367.46
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结构图
CAS No: 1426683-30-8
产品详情
生物活性：
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
体外研究：
The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site.
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
体外研究：
The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site.
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