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ADH-6 TFA
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 TFA图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

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 humancancercells, which restores p53's transcriptional activity, leading to cell cycle arrest andapoptosis. ADH-6 TFA has the potential for the research ofcancerdiseases[1].

体外研究
(In Vitro)

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.
体内研究
(In Vivo)

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
分子量

754.67

性状

Solid

Formula

C31H37F3N8O11

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(132.51 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.3251 mL6.6254 mL13.2508 mL
5 mM0.2650 mL1.3251 mL2.6502 mL
10 mM0.1325 mL0.6625 mL1.3251 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。