PF 06465469

Name: PF 06465469
Brand: Tocris Bioscience
SKU: 4710

Tocris Bioscience, part of Bio-Techne | Catalog # 4710

Citations (3)

COA / SDS

Potent ITK inhibitor; also inhibits BTK

Key Product Details

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)
Molecular Weight:	523.63

View Full Technical Details for PF 06465469

Technical Data
Citations

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 for PF 06465469

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	19.10 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 Covalent inhibitors of interleukin-2 inducible T cell kinase (Itk) with nanomolar potency in a whole-blood assay. J.Med.Chem. 2012 PMID: 23098091