Ravoxertinib (GDC-0994) is potent, selective and orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively. Ravoxertinib (GDC-0994) displays at least 50-fold selectivity against the Invitrogen Selectscreen panel containing 279 kinases. Ravoxertinib (GDC-0994) potently inhibits ERK dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with IC50 of 12 nM. Ravoxertinib (GDC-0994) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006). Ravoxertinib (GDC-0994) (15, 30, or 100 mg/kg, PO, QD) inhibits tumor growth in the HCT116 mouse xenograft model.
