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KI2575PF0646546910 mg$611
PF0646546950 mg$2535

Chemical Characteristic

Product NamePF06465469
CAS No.1407966-77-1
Molecular Weight 523.63
FormulaC30H33N7O2
Chemical Name(R)-3-[1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-isopropyl-5-methylphenyl)benzamide
SmilesC(=O)(c1cc(ccc1)c1c2c(ncnc2N)n(n1)C1CN(CCC1)C(=O)C=C)Nc1ccc(c(c1)C)C(C)C
Chemical Structure

Biological activities

PF-06465469 is a potent inhibitor of interleukin-2 inducible T cell kinase (ITK). The IC50 of PF-06465469 against ITK is 2 nM. PF-06465469 also shows inhibitory activity against Bruton's tyrosine kinase (BTK) with an IC50 of 2 nM. In vitro, PF-06465469 shows nanomolar potencies in a cell-based IP1 assay and human whole blood assay with IC50s of 31 and 48 nM, respectively.[1]

Protocols

In vitro, PF-06465469 is dissolved in DMSO.[1]

References

[1] Zapf CW, et al. Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay. J Med Chem. 2012, 55 (22): 10047-10063.

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