FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC₅₀ values in the low micromolar range^[1].

1.6 μM (pre-incubation 5 min ATP 0.5 μM), 1.3 μM (pre-incubation 60 min ATP 0.5 μM), 3.0 μM (pre-incubation 5 min ATP 1000 μM), 1.0 μM (pre-incubation 60 min ATP 1000 μM).

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^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

367.46

C₂₀H₂₁N₃O₂S

1426683-30-8

Room temperature in continental US; may vary elsewhere.

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• [1]. Iwatani M, et al. Discovery and characterization of novel allosteric FAK inhibitors. Eur J Med Chem. 2013 Mar;61:49-60.