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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).


| Description | 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). |
| Targets&IC50 | ERK2:3.1 nM, p-RSK:12 nM, ERK1:6.1 nM |
| In vitro | 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]. |
| In vivo | 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]. |
| Synonyms | GDC-0994 (hydrochloride) |
| Molecular Weight | 477.32 |
| Formula | C21H19Cl2FN6O2 |
| Cas No. | 2070009-58-2 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (209.5 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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