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. 2018 Jul 16;23(9):919–929. doi: 10.1177/2472555218786165

Figure 5.

Figure 5.

Assay utility in CLL and DLBCL patient samples: (A) PBMCs, (B) lymph nodes, and (C) bone marrow. (A) The concentration of total BTK in PBMCs from nine patients with CLL ranged from 33 to 174 ng/mL. The average total BTK expression in PBMCs from four healthy volunteers (HV, gray bar) was 30 ng/mL. Data represent the average and standard error of quadruplicate samples from each subject or from four healthy donors tested in quadruplicate. (B) The TR-FRET assay detected robust levels of free (light blue bars) and total (dark blue bars) BTK in lymph node (LN) tissue lysates from two patients with DLBCL. Data represent the average and standard error from samples tested in triplicate. (C) Matched BMMCs and PBMCs from two patients with CLL were treated by spiking 110, 8, and 0.1 nM tirabrutinib with a final DMSO concentration of 0.1%. The TR-FRET assay showed dose-dependent BTK binding after ex vivo treatment with tirabrutinib. BTK occupancy reached nearly 100% at a dose of 110 nM tirabrutinib. Data represent the average and standard error from triplicate samples.