Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).

Ravoxertinib inhibits p90RSK (IC50: 12 nM) [1]. Ravoxertinib is highly selective for ERK1 and ERK2 (biochemical potency: 1.1 nM and 0.3 nM, respectively) [2].

Ravoxertinib (10 mg/kg; p.o.; in CD-1 mice) is sufficient to achieve the desired target coverage for at least 8 h [1]. Ravoxertinib (p.o.; daily) causes significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice [2].

2070009-58-2

C21H19Cl2FN6O2

477.32

GDC-0994 (hydrochloride);Ravoxertinib hydrochloride

DMSO:100 mg/mL (209.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years