Ibrutinib

Biological Activity

Ibrutinib is a potent and selective BTK inhibitor (IC₅₀= 0.5 nM). Selective for BTK against a screening panel of kinase enzymes. Inhibits autophosphorylation of BTK, phosphorylation of PLCγ, and phosphorylation of ERK (IC₅₀ of 11 nM, 29 nM and 13 nM, respectively). Also inhibits ErbB4 (IC₅₀ = 0.25-3.4 nM). Induces cytotoxicity of chronic lymphocytic leukemia (CLL) cells. Reduces clinical arthritis scores in a mouse model.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy.
   Honigberg et al.
   Proc.Natl.Acad.Sci.U.S.A., 2010;107:13075
2. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase.
   Pan et al.
   Chem.Med.Chem., 2007;2:58

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