Network Version
Ravoxertinib Data Sheet
| Product Name: | Ravoxertinib |
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| CAS No.: | 1453848-26-4 | |
| Cat. No.: | HY-15947 | |
| MWt: | 440.86 | |
| Formula: | C21H18ClFN6O2 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 35 mg/mL | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an 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 (GDC-0994) also inhibits p90RSK with an IC50 of 12 nM[1]. Ravoxertinib (GDC-0994) 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)[3]. In Vivo: In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib (GDC-0994) 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]. |
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