Ravoxertinib hydrochloride (C09-1167-790)

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC 50 of 6.1 nM and 3.1 nM for ERK1 and ERK2 , respectively.In VitroRavoxertinib 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoIn 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:ERK2 3.1 nM (IC 50 ) ERK1 6.1 nM (IC 50 ) p-RSK 12 nM (IC 50 ). Specifications and Purity: 98%. Molecular Formula: C21H19Cl2FN6O2. Molecular Weight: 477.32. PubChem CID: 92044395. Isomeric SMILES: CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)[C@H](CO)C4=CC(=C(C=C4)Cl)F.Cl.