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。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
2mg

￥1100.00

880.00

- +
5mg

￥1625.00

1300.00

- +
10mg

￥2812.00

2250.00

- +
50mg

￥8100.00

6480.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

Background

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.