CS-2072

Ravoxertinib also inhibits p90RSK with IC ₅₀ of 12 nM.
Ravoxertinib is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively.
Ravoxertinib (GDC0994; 50 nM, 0.5 µM, and 5 µM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006).

In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib is sufficient to achieve the desired target coverage for at least 8 h. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice.