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. 2022 Nov 13;114(2):654–664. doi: 10.1111/cas.15617

FIGURE 3.

FIGURE 3

Pharmacokinetics and pharmacodynamics of TAS2940 in NCI‐N87 mouse xenograft model. (A) Plasma concentration profiles of TAS2940 after a single oral treatment (left panel) or multiple oral treatments for 7 days (right panel) in male BALB/cAJcl‐nu/nu mice. Data are shown as the mean + SD (n = 3). (B–D) Inhibition of phospho‐human epidermal growth factor receptor type 2 (HER2), HER3, and their downstream molecules by TAS2940 was evaluated in NCI‐N87 nude mouse xenograft model by western blot analysis. Using the samples collected at 1 h following treatment with TAS2940 at various concentrations, the chemiluminescence signal bands for phospho‐HER2, HER2 protein, phospho‐HER3, HER3 protein, and β‐actin in (C) were subjected to semiquantitative analysis, and the phospho‐HER2/HER2 and phospho‐HER3/HER3 signal ratios were calculated (B). Duration of inhibitory activity against HER2 signaling was confirmed after treatment with TAS2940 at 25.0 mg/kg (D).