Fig. 5

BBB permeability and in vivo activity. a–b Female NPG mice were implanted with MCF-7 cells intracranially. Eight days after tumor cell implantation (designated as Day 0 of the study), mice were treated with vehicle, 250 mg/kg fulvestrant (administration as described above), 3 or 10 mg/kg SCR-6852 (QD, n = 8/group), and survival of the animals were recorded. The survival curves of the animals are shown (a). Representative images of the brain tissue H&E staining are also shown (b). The day that the brain tissues were collected for the representative images is indicated in the graph. Scale bar: 3 mm or 300 μm. c The intracranial MCF7 (orthotopic) xenograft mice were treated with SCR-6852 or Fulvestrant for 8 days, and the tissues were collected 24 h after the last dose. SCR-6852 or Fulvestrant concertation in the brain or plasma was determined by LC–MS. Brain conc./plasma conc. was presented as a B/P ratio. d The CD1 IGS mice/rat / Beagle were administrated with multiple doses of SCR-6852 or other compounds, and the tissues were collected at 24 h after the last dose as described in methods. relative compound concertation in the brain or plasma was determined by LC–MS. Brain conc./plasma conc. was presented as a B/P ratio