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  • Ravoxertinib hydrochloride
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Ravoxertinib hydrochloride

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) 是一种可口服的 ERK 抑制剂,对 ERK1 和 ERK2 的 IC50 值分别为 6.1 nM 和 3.1 nM。

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¥1100-8100
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880-6480
Ravoxertinib hydrochloride的二维码

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  • 货号: ajce58384
  • CAS: 2070009-58-2
  • 别名: GDC-0994 hydrochloride
  • 分子式: C21H19Cl2FN6O2
  • 分子量: 477.32
  • 纯度: >98%
  • 溶解度: DMSO: 100 mg/mL (209.50 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively. ERK2|3.1 nM (IC50)|ERK1|6.1 nM (IC50)|p-RSK|12 nM (IC50)


Ravoxertinib also inhibits p90RSK with IC50 of 12 nM[1]. Ravoxertinib is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively[2].


In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib 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].


[1]. Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developme [2]. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.

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