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. 2024 Apr 19;14(7):1190–1205. doi: 10.1158/2159-8290.CD-24-0139

Figure 6.

Figure 6.

NST-628 is a fully brain-penetrant inhibitor. A,In vivo half-life, rat brain Kp, Kp, uu, and mouse Kp values for NST-628, trametinib, and avutometinib. B, Plasma concentration compared with phospho-ERK levels 4 hours after dose in normal mouse brains of mice treated with 1 mg/kg trametinib, 1 mg/kg avutometinib, 5 mg/kg cobimetinib, or 0.3, 1, or 3 mg/kg NST-628. C, Bioluminescent imaging of SK-MEL-2-luc intracranial tumors treated with vehicle or 1.5 mg/kg b.i.d. NST-628 at D0, D7, and D18 of the study. D, Intracranial tumor volume measured by bioluminescent imaging of SK-MEL-2-luc tumors treated with 0.3 mg/kg qd trametinib, 0.3 mg/kg qd avutometinib, 3 mg/kg qd or 1.5 mg/kg b.i.d. NST-628. E, Tumor volume as measured by bioluminescent imaging of intracranial MeWo-luc tumors treated with 25 mg/kg qd tovorafenib or 0.3, 1, 3 mg/kg qd NST-628. F, DUSP6 transcript levels in intracranial MeWo-luc tumors treated with 25 mg/kg tovorafenib or 3 mg/kg NST-628 at 4, 8, and 24 hours after single dose of inhibitor.