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ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity,
In Vitro:ADH-6 (25 μM, 10 h) TFA inhibits aggregation of pR248W (indicated by dot blot assay). ADH-6 (5 μM, 6 h) TFA dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells. ADH-6 (0-10 μM, 24 or 48 h) TFA causes selective cytotoxicity in can
In Vivo:ADH-6 (intraperitoneal injection, 15mg/kg, every 2 days, for a total of 12 doses) TFA causes regression of mutant p53-bearing tumors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MIA P
Biological Activity:ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity,