产品
编 号:F167841
分子式:C21H18ClFN6O2
分子量:440.86
产品类型
结构图
CAS No: 1453848-26-4
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产品详情
生物活性:
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.
体内研究:
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. 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.
体外研究:
Ravoxertinib (GDC-0994) also inhibits p90RSK with an IC50 of 12 nM. Ravoxertinib (GDC-0994) 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).