PF 06465469

Pricing Availability Delivery Time Qty
Cat.No. 4710 - PF 06465469 | C30H33N7O2 | CAS No. 1407966-77-1
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
Literature

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.

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

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Product Datasheets

Safety Datasheet

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


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Citations for PF 06465469

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