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.
Technical Data
| M. Wt | 523.63 |
| Formula | C30H33N7O2 |
| Storage | Store at +4°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 1407966-77-1 |
| PubChem ID | 71450146 |
| InChI Key | CGJVMKJGKFEHTL-HSZRJFAPSA-N |
| Smiles | NC1=C2C(N([C@@H]4CCCN(C(C=C)=O)C4)N=C2C3=CC(C(NC5=CC(C)=C(C(C)C)C=C5)=O)=CC=C3)=NC=N1 |
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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Zapf et 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
Keywords: PF 06465469, supplier, PF06465469, Pfizer, interleukin-2, IL-2, inducible, T, cell, kinase, ITK, inhibitors, inhibits, potent, Brutons, tyrosine, kinase, BTK, Brutons, Tyrosine, Kinase, (BTK), ITK, ITK, Tocris Bioscience
