Pricing Availability   Qty
Description: Potent and selective BTK inhibitor
Chemical Name: 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for Ibrutinib

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.

Compound Libraries for Ibrutinib

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.

Technical Data for Ibrutinib

M. Wt 440.5
Formula C25H24N6O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 936563-96-1
PubChem ID 24821094
Smiles NC1=C2C(N([C@@H]3CCCN(C(C=C)=O)C3)N=C2C4=CC=C(C=C4)OC5=CC=CC=C5)=NC=N1

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.

Solubility Data for Ibrutinib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 44.05 100

Preparing Stock Solutions for Ibrutinib

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.

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

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Product Datasheets for Ibrutinib

Certificate of Analysis / Product Datasheet
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References for Ibrutinib

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

If you know of a relevant reference for Ibrutinib, please let us know.

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1 Citation for Ibrutinib

Citations are publications that use Tocris products. Selected citations for Ibrutinib include:

John E et al (2021) Ibrutinib as a potential therapeutic for cocaine use disorder. Transl Psychiatry 11 623 PMID: 34880215

Do you know of a great paper that uses Ibrutinib from Tocris? Please let us know.

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