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Ravoxertinib

CAS No. : 1453848-26-4

MCE 站：Ravoxertinib

产品活性：Ravoxertinib (GDC-0994) 是具有口服活性的 ERK 激酶抑制剂，抑制 ERK1 和 ERK2 的IC₅₀ 分别为6.1 nM 和 3.1 nM。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt

作用靶点：ERK

In Vitro: 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 ?M, and 5 ?M; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006).

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. 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.

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