PF 06465469

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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)
Datasheet
Citations (2)
Reviews

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.

Select a batch to recalculate based on the batch molecular weight:
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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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


If you know of a relevant reference for PF 06465469, please let us know.

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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:

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

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


Do you know of a great paper that uses PF 06465469 from Tocris? Please let us know.

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