Ibrutinib

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Cat.No. 6813 - Ibrutinib | C25H24N6O2 | CAS No. 936563-96-1
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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). Induces cytotoxicity of chronic lymphocytic leukemia (CLL) cells. Reduces clinical arthritis scores in a mouse model.

Technical Data

M. Wt 440.5
Formula C25H24N6O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 936563-96-1
PubChem ID 24821094
InChI Key XYFPWWZEPKGCCK-GOSISDBHSA-N
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

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

Preparing Stock Solutions

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

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References

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


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Citations for Ibrutinib

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