Ravoxertinib hydrochloride

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with 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 also inhibits p90RSK with IC₅₀ of 12 nM^[1].
Ravoxertinib is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively^[2].
Ravoxertinib (GDC0994; 50 nM, 0.5 µM, and 5 µM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006)^[4]. In Vivo: 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^[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].