PF-303 

PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC₅₀=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation^[1][2].

436.89

C₂₂H₂₁ClN₆O₂

1609465-78-2

NC(C1=C(N)N([C@H]2CN(CCC2)C#N)N=C1C3=CC=C(C=C3)OC4=CC=C(C=C4)Cl)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Benson M J, et al. Modeling the clinical phenotype of BTK inhibition in the mature murine immune system[J]. The Journal of Immunology, 2014, 193(1): 185-197.  [Content Brief]

  [2]. Schnute M E, et al. Aminopyrazole carboxamide bruton’s tyrosine kinase inhibitors. irreversible to reversible covalent reactive group tuning[J]. ACS Medicinal Chemistry Letters, 2018, 10(1): 80-85.  [Content Brief]