ADH-6 TFA 是一种三吡啶酰胺化合物。ADH-6 TFA 消除了突变 p53 DBD 的聚集成核亚结构域的自组装。ADH-6 TFA 靶向并解离人类癌细胞中的突变 p53 聚集体，从而恢复 p53 的转录活性，导致细胞周期停滞和细胞凋亡 (apoptosis)。ADH-6 TFA 具有研究癌症疾病的潜力。
| 分子式 | C31H37F3N8O11 |
| 分子量 | 754.67 |
| 溶解度 | DMSO : 100 mg/mL (132.51 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases[1]. ADH-6 (25 μM, 10 h) TFA inhibits aggregation of pR248W (indicated by dot blot assay)[1].
ADH-6 (5 μM, 6 h) TFA dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells[1].
ADH-6 (0-10 μM, 24 or 48 h) TFA causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2)[1].
ADH-6 (5 μM, 24 h) TFA specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells[1].
Cell Viability Assay[1] | Cell Line: | MIA PaCa-2 (mutant R248W p53), SK-BR-3 (mutant R175H p53) | | Concentration: | 0, 2.5, 5, 7.5, 10 μM | | Incubation Time: | 24, 48 h | | Result: | Caused death of cancer cells bearing mutant, but not WT, p53. |
Western Blot Analysis[1] | Cell Line: | MIA PaCa-2 cells | | Concentration: | 5 μM | | Incubation Time: | 24 h | | Result: | Increased expression of p53-inducible MDM2 and proapoptotic Bax. |
ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) TFA 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. |
| 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 |
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