FAK inhibitor 5

Modify Date: 2024-01-12 07:14:37

FAK inhibitor 5 Structure
FAK inhibitor 5 structure
Common Name FAK inhibitor 5
CAS Number 1426683-30-8 Molecular Weight 367.46
Density N/A Boiling Point N/A
Molecular Formula C20H21N3O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of FAK inhibitor 5


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

 Names

Name FAK inhibitor 5

 FAK inhibitor 5 Biological Activity

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

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).

In Vitro 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].
References

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

 Chemical & Physical Properties

Molecular Formula C20H21N3O2S
Molecular Weight 367.46