PCI 29732 serves as a highly effective, orally bioavailable, and reversible inhibitor of BTK, displaying Kiapp values of 8.2 nM for BTK, 4.6 nM for Lck, and 2.5 nM for Lyn. Its inhibitory effect on Itk, another member of the Tec family kinases, is relatively modest. Moreover, PCI 29732 disrupts the activity of ABCG2 by competitively attaching to its ATP-binding site[1].[2].
体内研究
Additionally, by competitively binding to the ATP-binding site of ABCG2, PCI 29732 not only inhibits ABCG2's function but also boosts the anti-tumor effects of chemotherapeutic agents that are substrates of ABCG2[2].
When administered at a dose of 20 mg/kg orally every three days for a total of five times, PCI 29732 significantly augments the anti-cancer performance of Topotecan in a H460/MX20 cell xenograft model in nude mice[2].
体外研究
PCI 29732 demonstrates cytotoxic properties across a variety of cell lines, with IC50 values reported as 7.94 μM for S1 cells, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells[2].
PCI-29732 effectively prevents the transcriptional activation of various B-cell activation genes in human CD20+ B cells following stimulation through the B-cell antigen receptor (BCR)[3].
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