PF 06465469 Discontinued See A191400 Chemical Properties

Melting point:

209-212°C

Boiling point:

730.2±60.0 °C(Predicted)

Density 

1.30±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble5mg/mL, clear

pka

12.83±0.70(Predicted)

form 

powder

color 

white to beige

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36/37

WGK Germany 

3

PF 06465469 Discontinued See A191400 Usage And Synthesis

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).

storage

Store at +4°C