Description: Potent ITK inhibitor; also inhibits BTK
Chemical Name: (R)-3-(1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(3-methyl-4-(1-methylethyl))benzamide
Purity: ≥95% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent inhibitor of interleukin-2 inducible T cell kinase (ITK) (IC50 = 2 nM). Also exhibits inhibitory activity against Bruton's tyrosine kinase (BTK) (IC50 = 2 nM). Displays nanomolar potencies in a cell-based IP1 assay and human whole blood assay (IC50 values are 31 and 48 nM respectively).
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
2.62
5mM with gentle warming
Preparing Stock Solutions
The following data is based on the product molecular weight 523.63. Batch specific molecular weights may vary from batch to batch due to solvent 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
1.91 mL
9.55 mL
19.1 mL
5 mM
0.38 mL
1.91 mL
3.82 mL
10 mM
0.19 mL
0.95 mL
1.91 mL
50 mM
0.04 mL
0.19 mL
0.38 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Zapfet al (2012) Covalent inhibitors of interleukin-2 inducible T cell kinase (Itk) with nanomolar potency in a whole-blood assay. J.Med.Chem. 55 10047 PMID: 23098091