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. 2022 Jul 12;65(14):9858–9872. doi: 10.1021/acs.jmedchem.2c00505

Figure 8.

Figure 8

Nectin-4/CD137 Bicycle TICA cause tumor regression in vivo. (A) Jurkat-CD137 reporter cells were cocultured with CT26 clone overexpressing Nectin-4 (CT26-Nectin-4) and treated with BCY10572 (1:1 Bicycle TICA), BCY11863 (1:2 Bicycle TICA), or CD137L. Data are mean ± s.d. (n ≥ 3 replicates). (B) Plasma concentration of BCY10572 and BCY11864 when dosed at 15 mg/kg by intraperitoneal injection to CD-1 mouse. (C, D) CT26-Nectin-4 tumor-bearing huCD137-Balb/c (C) or wild type Balb/c (D) mice were treated with daily doses of vehicle or BCY10572 (1 or 5 mg/kg) and tumor growth was monitored. Data are mean ± standard error of the mean (SEM) (n = 5 mice/treatment cohort). TV: tumor volume.