1. Protein Tyrosine Kinase/RTK
  2. FAK
  3. FAK inhibitor 5

FAK inhibitor 5 

Cat. No.: HY-18928
Handling Instructions

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

For research use only. We do not sell to patients.

FAK inhibitor 5 Chemical Structure

FAK inhibitor 5 Chemical Structure

CAS No. : 1426683-30-8

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Description

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

IC50 & 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].

Molecular Weight

367.46

Formula

C₂₀H₂₁N₃O₂S

CAS No.

1426683-30-8

SMILES

CCC1=CC=C(C2=CC=C3C(C4=C(S(=O)(N3C)=O)C=NN4CC)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

FAK inhibitor 5FAK inhibitor5FAK inhibitor-5FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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FAK inhibitor 5
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