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Submit ReviewPF 06465469
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 for PF 06465469
PF 06465469 is a 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 for PF 06465469
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PF 06465469
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 2.62 | 5 with gentle warming |
Preparing Stock Solutions for PF 06465469
The following data is based on the product molecular weight 523.63. 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 |
|---|---|---|---|
| 0.05 mM | 38.19 mL | 190.97 mL | 381.95 mL |
| 0.25 mM | 7.64 mL | 38.19 mL | 76.39 mL |
| 0.5 mM | 3.82 mL | 19.1 mL | 38.19 mL |
| 2.5 mM | 0.76 mL | 3.82 mL | 7.64 mL |
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Product Datasheets for PF 06465469
References for PF 06465469
References are publications that support the biological activity of the product.
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
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Keywords: PF 06465469, PF 06465469 supplier, PF06465469, Pfizer, interleukin-2, IL-2, inducible, T, cell, kinase, ITK, inhibitors, inhibits, potent, Brutons, tyrosine, BTK, Tyrosine, Kinase, (BTK), 4710, Tocris Bioscience
2 Citations for PF 06465469
Citations are publications that use Tocris products. Selected citations for PF 06465469 include:
Mamand et al (2018) Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma. Sci Rep 8 14216 PMID: 30242208
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
Do you know of a great paper that uses PF 06465469 from Tocris? Please let us know.
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