ADH-6 TFA|西域试剂

ADH-6 TFA,99.91%

产品编号：Bellancom-145785A| 分子式：C₃₁H₃₇F₃N₈O₁₁| 分子量：754.67

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-145785A		￥5800.00	杭州北京（现货）
Bellancom-145785A		￥10500.00	杭州北京（现货）

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ADH-6 TFA

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 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.

体外研究

ADH-6 (25 μM, 10 h) TFA inhibits aggregation of pR248W (indicated by dot blot assay).
ADH-6 (5 μM, 6 h) TFA dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells.
ADH-6 (0-10 μM, 24 or 48 h) TFA causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2).
ADH-6 (5 μM, 24 h) TFA specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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 .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	C_max: 21 µg/mL, T_1/2: 3.6 h

体内研究

ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) TFA causes regression of mutant p53-bearing tumors .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	C_max: 21 µg/mL, T_1/2: 3.6 h

体内研究

ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) TFA causes regression of mutant p53-bearing tumors .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	C_max: 21 µg/mL, T_1/2: 3.6 h

性状

Solid

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 mg	5 mg	10 mg

1 mM	1.3251 mL	6.6254 mL	13.2508 mL
5 mM	0.2650 mL	1.3251 mL	2.6502 mL
10 mM	0.1325 mL	0.6625 mL	1.3251 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式