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(R)-2-(6,8-Dibromo-2-oxo-2H-chromene-3-carboxamido)-5-(ethylamino)-5-oxopentanoic Ethyl Ester

Development stage
Preclinical
Modality
Small Molecules
01

Overview

DTBrC, or (R)-2-(6,8-Dibromo-2-oxo-2H-chromene-3-carboxamido)-5-(ethylamino)-5-oxopentanoic Ethyl Ester, is a semisynthesized derivative of theanine. It is being investigated for its anticancer activities, particularly in human hepatocellular carcinoma (HHC). DTBrC has demonstrated inhibitory effects on the growth and migration of HHC cells in various models (in vitro, ex vivo, and in vivo). It also enhances the repression of HHC cell growth when combined with the anticancer drug pirarubicin. Its mechanism of action involves repressing the protein expressions in the Met/EGFR/VEGFR-Akt/NF-κB signaling pathways and enhancing p53 protein expression.

02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)MET (Mesenchymal-epithelial transition factor receptor)NFKB1 (NF-κB1)TP53 (Cellular Tumor Antigen p53 R175H)EGFR T790M (Epidermal growth factor receptor T790M mutant)VEGFR (VEGFR family)

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