Title : AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib.

Pub. Date : 2021 Feb

PMID : 33273059






2 Functional Relationships(s)
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1 In vitro, AZD0364 treatment resulted in inhibition of proximal and distal biomarkers and reduced proliferation in sensitive BRAF mutant and KRAS mutant cell lines. N-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide B-Raf proto-oncogene, serine/threonine kinase Homo sapiens
2 In multiple in vivo xenograft models, AZD0364 showed dose and time-dependent modulation of ERK1/2-dependent signalling biomarkers resulting in tumour regression in sensitive BRAF and KRAS mutant xenografts. N-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide B-Raf proto-oncogene, serine/threonine kinase Homo sapiens