Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Ravoxertinib hydrochloride
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2070009-58-2

2070009-58-2 structure

2070009-58-2 structure

Name: Ravoxertinib hydrochloride
Chemical Name: GDC-0994 hydrochloride
CAS Number: 2070009-58-2
Molecular Formula: C₂₁H₁₉Cl₂FN₆O₂
Molecular Weight: 477.32
Catalog: Research Areas Cancer
Create Date: 2018-04-21 08:44:57
Modify Date: 2024-01-11 21:09:36
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.

Name	GDC-0994 hydrochloride
Synonyms	GDC-0994 (hydrochloride)

Description	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.
Related Catalog	Research Areas >> Cancer
Target	ERK2:3.1 nM (IC50) ERK1:6.1 nM (IC50) p-RSK:12 nM (IC50)
In Vitro	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 Vivo	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].
Animal Admin	Mice[1] PK/PD data for Ravoxertinib in the HCT116 mouse xenograft model. HCT116 tumors are established in nude mice to a tumor volume of 400−600 mm3. Mice are treated with a single oral dose of 22 at 15, 30, or 100 mg/kg versus vehicle control alone (40% PEG400/60% (10% HPβCD)) follow by tumor and plasma collection at 2, 8, 16, and 24 h postdose. Tumor levels of phosphorylated p90RSK (pRSK) relative total p90RSK (tRSK) are measured by quantitative Western blot and are normalized to vehicle control at 2 h postdose (set to 100%). Plasma and tumor concentrations are measured by LC−MS.
References	[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.

Molecular Formula	C₂₁H₁₉Cl₂FN₆O₂
Molecular Weight	477.32