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CAS No.: 1054543-47-3

Apoptozole Catalog No. CSN18941

Synonyms: Apoptosis Activator VII

Apoptozole is an inhibitor of heat shock protein 70 (HSP70) and Hsc70. It induces caspase-dependent apoptosis.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述HSC70 and HSP70 are the two major cytosolic isoforms of the HSP70 family. Between this two proteins, HSP70 is present at relatively low levels in normal cells but can be elevated in expression to protect cells from apoptosis in response to various stressful stimuli such as anticancer agents, especially the HSP90 inhibitors, making it become an important target for anticancer therapy due to its antiapoptotic and oncogenic functions. Apoptozole is a dual HSC70 and HSP70 inhibitor with Kd values of 0.21μM and 0.14μM (measured by SPR spectroscopy), which can potently induced apoptosis in P19 and A549 cells up to 90% at concentration of 1μM for 12h^[1]. This strong potency of Apoptozole to apoptosis induction may due to its effect on disrupting the interaction of HSP70 with APAF-1, which can be bound with by HSP70 and halt the progression of the caspase-dependent apoptotic pathway. Intraperitoneal injection with Apoptozole at dose of 4mg/kg/day every other day for 2 weeks could significantly reduce tumor growth of the A549, RKO, and HeLa xenografts up to 61%, 65% and 68%. Combined treatment of Apoptozole with Doxorubicin can enhance the potency of the agent alone^[2].
作用机制Apoptozole can bind to the ATPase domain of HSP70 and block its ATPase activity.^[1]

动物研究

剂量

Mice^[2] (i.p.): 4 mg/kg, 10 mg/kg

给药途径

i.p.

动物药代数据

Animal	Mice^[2]
Dose	10 mg/kg
Administration	i.p.
T_1/2	8.04 h
T_max	1 h
C_max	2159.13 ± 278.25 mg/l
AUC_0→∞	10951.73 mg·h/l
MRT_0→∞	7.9 h
AUC_0→t	9969.93 mg·h/l

参考文献

[1] Williams DR, Ko SK, et al. An apoptosis-inducing small molecule that binds to heat shock protein 70. Angew Chem Int Ed Engl. 2008;47(39):7466-9.
[2] Ko SK, Kim J, et al. A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities. Chem Biol. 2015 Mar 19;22(3):391-403.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5986 mL
- 7.9928 mL
- 15.9857 mL
- 5 mM
- 0.3197 mL
- 1.5986 mL
- 3.1971 mL
- 10 mM
- 0.1599 mL
- 0.7993 mL
- 1.5986 mL

技术信息

CAS号

1054543-47-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H25F6N3O3

运输

蓝冰

分子量

625.56

别名

Apoptosis Activator VII

溶解度

DMSO	50.0 mg/mL (79.9 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

5 mg/mL

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