| Identification | Back Directory | [Name]
2-Pyridinecarboxylic acid, 6-(3-aminopropoxy)-5-[[[6-(3-aminopropoxy)-5-[[(6-butoxy-5-nitro-2-pyridinyl)carbonyl]amino]-2-pyridinyl]carbonyl]amino]-, methyl ester | [CAS]
2227429-65-2 | [Synonyms]
2-Pyridinecarboxylic acid, 6-(3-aminopropoxy)-5-[[[6-(3-aminopropoxy)-5-[[(6-butoxy-5-nitro-2-pyridinyl)carbonyl]amino]-2-pyridinyl]carbonyl]amino]-, methyl ester | [Molecular Formula]
C29H36N8O9 | [MOL File]
2227429-65-2.mol | [Molecular Weight]
640.64 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) causes regression of mutant p53-bearing tumors [1].
| Animal Model: | MIA PaCa-2 xenografts[1] | | 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.
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| Animal Model: | MIA PaCa-2 xenografts (pharmacokinetics assay)[1] | | Dosage: | 15 mg/kg | | Administration: | Intraperitoneal injection, for a single dose | | Result: | Cmax: 21?μg/mL, T1/2: 3.6 h |
| [References]
[1] Palanikumar L, et al. Protein mimetic amyloid inhibitor potently abrogates cancer-associated mutant p53 aggregation and restores tumor suppressor function. Nat Commun. 2021;12(1):3962. DOI:10.1038/s41467-021-23985-1 |
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