产品
编 号：F750056
分子式：C29H36N8O9
分子量：640.64
分子式：C29H36N8O9
分子量：640.64
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CAS No: 2227429-65-2
产品详情
生物活性：
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases.
体内研究：
ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) causes regression of mutant p53-bearing tumors .Animal Model:MIA PaCa-2 xenografts
Dosage:716.4?μM in 0.02% DMSO
Administration:Intraperitoneal injection, every 2 days, for a total of 12 doses
Result:Reduced tumor growth relative to the saline-treated control group.Reduced mutant p53 levels and shrinked xenografts harboring aggregation-prone mutant p53.
Animal Model:MIA PaCa-2 xenografts (pharmacokinetics assay)
Dosage:15 mg/kg
Administration:Intraperitoneal injection, for a single dose
Result:Cmax: 21?μg/mL, T1/2: 3.6 h
体外研究：
ADH-6 (25 μM, 10 h) inhibits aggregation of pR248W (indicated by dot blot assay).ADH-6 (5 μM, 6 h) dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells.ADH-6 (0-10 μM, 24 or 48 h) causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2).ADH-6 (5μM, 24 h) specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells.
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases.
体内研究：
ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) causes regression of mutant p53-bearing tumors .Animal Model:MIA PaCa-2 xenografts
Dosage:716.4?μM in 0.02% DMSO
Administration:Intraperitoneal injection, every 2 days, for a total of 12 doses
Result:Reduced tumor growth relative to the saline-treated control group.Reduced mutant p53 levels and shrinked xenografts harboring aggregation-prone mutant p53.
Animal Model:MIA PaCa-2 xenografts (pharmacokinetics assay)
Dosage:15 mg/kg
Administration:Intraperitoneal injection, for a single dose
Result:Cmax: 21?μg/mL, T1/2: 3.6 h
体外研究：
ADH-6 (25 μM, 10 h) inhibits aggregation of pR248W (indicated by dot blot assay).ADH-6 (5 μM, 6 h) dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells.ADH-6 (0-10 μM, 24 or 48 h) causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2).ADH-6 (5μM, 24 h) specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells.
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