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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.
Ibrutinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Epigenetics Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 440.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.27 mL||11.35 mL||22.7 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|
References are publications that support the biological activity of the product.
Honigberg et al (2010) 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 107 13075 PMID: 20615965
Pan et al (2007) Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. Chem.Med.Chem. 2 58 PMID: 17154430
Estupiñán et al (2021) Comparative analysis of BTK inhibitors and mechanisms underlying adverse effects. Front.Cell Dev.Biol. 9 630942 PMID: 33777941
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Keywords: Ibrutinib, Ibrutinib supplier, Potent, and, selective, Bruton, tyrosine, kinase, inhibitor, Btk, Brutons, Tyrosine, Kinase, (BTK), EGFR, 6813, Tocris Bioscience
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