Fig. 3: Pro-BA shows enhanced antitumor activity compared to the corresponding degraders with linkers in vivo.

A H3122 cells were grafted into the right flank of 4-week-old female nude mice. The mice were treated with vehicle, Brigatinib, Pro-PEG3-BA, or Pro-BA at dose of 10 mg/kg, prepared in a solution of 90% corn oil + 10% DMSO via I.P. route every other day for a total of 8 administrations. Tumors were harvested from each group and photographed. B The bar graphs represent the mean ± SD of the primary tumor volumes of mice in (A). C The graph depicts the mean tumor growth of mice in (A), with treatment intervals marked by black arrows. D Analysis of EML4-ALK protein levels in tumor samples from (A) using immunoblotting. E Quantitative analysis of the Western blot results presented in (D). Data are presented as the mean ± SD (n = 5 mice per group). Statistical analysis was performed using one-way ANOVA followed by Fisher’s LSD test (two-tailed) for pairwise comparisons. F The graph illustrates the average body weight of mice receiving I.P. administration as described in (C). For (B), (C) data are presented as the mean ± SD (n = 5 mice per group). Statistical analysis was performed using Brown-Forsythe and Welch ANOVA followed by Welch’s t-tests (two-tailed) due to unequal variances (p < 0.05). Source data are provided as a Source Data file.