PF 06465469
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%
Biological Activity
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).Technical Data
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.
Additional Information
Background References
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Covalent inhibitors of interleukin-2 inducible T cell kinase (Itk) with nanomolar potency in a whole-blood assay.
Zapf et al.
J.Med.Chem., 2012;55:10047
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Citations for PF 06465469
The citations listed below are publications that use Tocris products. Selected citations for PF 06465469 include:
2 Citations: Showing 1 - 2
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Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL.
Authors: Christopher J Et al.
Cancer Res 2022;82:3375-3393
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Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma.
Authors: Mamand Et al.
Sci Rep 2018;8:14216
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