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NCi: An orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

Inn NameRavoxertinib
Lab CodesGDC-0994, RG-7842
Chemical Name1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-{2-[(1-methyl-1H-pyrazol-5-yl)amino]pyrimidin-4-yl}pyridin-2(1H)-one
Chemical StructureRavoxertinib.png
Molecular FormulaC21H18ClFN6O2
Cas Registry Number1453848-26-4
New Molecular EntityYes
OriginatorArray BioPharma
Mechanism Of ActionERK inhibitor
Who Atc CodesL01X-E (Protein kinase inhibitors)
Ephmra CodesL1H (Protein Kinase Inhibitor Antineoplastics)
IndicationNon-Small Cell Lung Cancer, Metastatic Colorectal Cancer, Metastatic Non Small Cell Lung Cancer, Metastatic Cancers, Melanoma

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