Ibrutinib

Product Description

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.

Solubility

Preparing Stock Solutions for Ibrutinib

The following data is based on the product molecular weight 440.50

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.27 mL	11.35 mL	22.70 mL
5 mM	0.45 mL	2.27 mL	4.54 mL
10 mM	0.23 mL	1.14 mL	2.27 mL
50 mM	0.05 mL	0.23 mL	0.45 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Pan Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. Chem.Med.Chem. 2007 PMID: 17154430
• Estupiñán Comparative analysis of BTK inhibitors and mechanisms underlying adverse effects. Front.Cell Dev.Biol. 2021 PMID: 33777941
• Honigberg The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc.Natl.Acad.Sci.USA 2010 PMID: 20615965