PCI-33380 is a potent and irreversible Bruton's Tyrosine Kinase (BTK) inhibitor with a fluorescent probe. PCI-33380 was designed based on the ibrutinib scaffold and has been used in both cellular and in vivo studies that demonstrated the connection between the inhibitor binding event and phenotypic readouts of cellular responses due to the inhibition of Btk functions. Furthermore, the use of fluorescent probes in clinical trials has played an important role in determining the appropriate dosage of drugs for patients.