Ravoxertinib hydrochloride (Synonyms: GDC-0994 hydrochloride) |
Katalog-Nr.GC37071 |
Ravoxertinib-Hydrochlorid (GDC-0994-Hydrochlorid) ist ein oral bioverfÜgbarer Inhibitor, der selektiv fÜr die ERK-Kinase-AktivitÄt mit IC50 von 6,1 nM und 3,1 nM fÜr ERK1 bzw. ERK2 ist.
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Cas No.: 2070009-58-2
Sample solution is provided at 25 µL, 10mM.
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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