Chemical Properties
Beige Solid
Uses
PF 06465469 is a covalent Inhibitors of Interleukin-2 Inducible T Cell Kinase (Itk) with nanomolar potency in a whole-blood assay.
Uses
(R)-3-[1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-isopropyl-5-methylphenyl)benzamide is a potential covalent inhibitor of Interleukin-2 Inducible T Cell KInase (Itk).
Itk is a member of the TEC-kinase family and is associated with the induction of T cell proliferation and drives cytokines through NFATc.
Biological Activity
PF-06465469 is a potent, covalent inhibitor of the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase), which is expressed primarily in immune cells, and is strongly upregulated following activation of T-cells. PF-06465469 inhibits Itk enzymatic activity with an IC50 of 2 nM. The compound blocks anti-CD3 induced phosphorylation of PLCg in Jurk at cells (IC50 = 31 nM) and IL-2 production in anti-CD3 stimulated human whole blood (IC50 = 48 nM).
