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Ravoxertinib hydrochloride

Catalog No. T15377 CAS 2070009-58-2

Synonyms: GDC-0994 (hydrochloride)

Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).

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Ravoxertinib hydrochloride Chemical Structure

Ravoxertinib hydrochloride, CAS 2070009-58-2

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Storage & Solubility Information

Description	Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).
Targets&IC50	p-RSK:12 nM, ERK2:3.1 nM, ERK1:6.1 nM
In vitro	Ravoxertinib inhibits p90RSK (IC50: 12 nM) [1]. Ravoxertinib is highly selective for ERK1 and ERK2 (biochemical potency: 1.1 nM and 0.3 nM, respectively) [2].
In vivo	Ravoxertinib (10 mg/kg; p.o.; in CD-1 mice) is sufficient to achieve the desired target coverage for at least 8 h [1]. Ravoxertinib (p.o.; daily) causes significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice [2].

Synonyms	GDC-0994 (hydrochloride)
Molecular Weight	477.32
Formula	C21H19Cl2FN6O2
CAS No.	2070009-58-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (209.50 mM), Sonication is recommended.

References and Literature

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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ravoxertinib hydrochloride 2070009-58-2 MAPK ERK GDC0994 GDC 0994 GDC-0994 (hydrochloride) GDC-0994 Ravoxertinib Hydrochloride inhibitor inhibit

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