tcsc3704 Ravoxertinib

Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC₅₀ of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

IC50 & Target: IC50: 6.1 nM (ERK1), 3.1 nM (ERK2), 12 nM (p90RSK)^[1]

In Vitro: Ravoxertinib (GDC-0994) also inhibits p90RSK with IC₅₀ of 12 nM^[1]. Ravoxertinib (GDC-0994) is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively^[2].

In Vivo: In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib (GDC-0994) is sufficient to achieve the desired target coverage for at least 8 h^[1]. 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^[2].