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ADH-6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ADH-6图片
CAS NO:2227429-65-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ADH-6 是一种三吡啶酰胺化合物。ADH-6 消除了突变 p53 DBD 的聚集成核亚结构域的自组装。ADH-6 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 具有研究癌症疾病的潜力。
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 humancancercells, which restores p53's transcriptional activity, leading to cell cycle arrest andapoptosis. ADH-6 has the potential for the research ofcancerdiseases[1].

体外研究
(In Vitro)

ADH-6 (25 μM, 10 h) inhibits aggregation of pR248W (indicated by dot blot assay)[1].
ADH-6 (5 μM, 6 h) dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells[1].
ADH-6 (0-10 μM, 24 or 48 h) causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2)[1].
ADH-6 (5 μM, 24 h) 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.
体内研究
(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.
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
分子量

640.64

Formula

C29H36N8O9

CAS 号

2227429-65-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.