Small molecule allosteric inhibitors of RORγt block Th17-dependent inflammation and associated gene expression in vivo
Fig 9
In vivo analysis of RORγt inhibitor activity on tumor growth.
Tumors were implanted in the flanks of C57Bl/6 mice and treatment began when average tumor volume reached 200 mm3. (A) Tumor volumes from animals treated with vehicle, Compound 3 alone, gemcitabine, Compound 3 plus gemcitabine or a positive control, cisplatin, were evaluated over 28 days of dosing. Averages were calculated from n = 8 mice per group. Error bars represent SEM. (B) Concentrations were measured by HPLC and plotted as mean ± SD. (C) qPCR expression analysis normalized to β-actin expression for vehicle, Compound 3, or Compound 3 plus gemcitabine treated tumor samples and plotted as mean ± SD.