Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Apoptozole (Apoptosis Activator VII) 是一种Hsc70和Hsp70的 ATPase 结构域抑制剂,可诱导凋亡,Kd 值分别为 0.21 和 0.14 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 279 | 现货 | ||
5 mg | ¥ 439 | 现货 | ||
10 mg | ¥ 628 | 现货 | ||
25 mg | ¥ 1,330 | 现货 | ||
50 mg | ¥ 2,620 | 现货 | ||
100 mg | ¥ 3,830 | 现货 | ||
200 mg | ¥ 5,480 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 672 | 现货 |
产品描述 | Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, and can induce apoptosis. |
靶点活性 | HSP70:0.14 μM(Kd), HSC70:0.21 μM(Kd) |
体外活性 | Apoptozole induces caspase dependent apoptosis by blocking interaction of HSP70 with APAF-1, without affecting interactions of HSP70 with ASK1, JNK, BAX, and AIF[2]. However, apoptozole may form aggregates under aqueous conditions that could interact with HSP70 proteins in a non-specific manner, potentially leading to false positives and inconsistent data[3]. |
体内活性 | Apoptozole greatly retards tumor growth in mice xenografted with cancer cells without affecting mouse viability. The elimination half-life time (T1/2) of Az in blood is found to be significantly longer than that of Dox (8.04 versus 1.60 hr) and the time needed to reach a maximum concentration (Tmax) of Az is shorter than that of Dox (1.00 versus 4.00 hr)[2]. |
激酶实验 | Inhibition of HER2/erbB2 tyrosine kinase activity: BT-474 cells are seeded on 24-well plates and cultured overnight. Mubritinib is then added at various concentrations. After incubation for 2 hours, the cells are harvested directly into sodium dodecyl sulfate (SDS)-sample buffer (200 μL). Aliquots containing equal amounts of total cell extract are run on 7.5% to 15% gradient SDS–polyacrylamide gel electrophoresis (PAGE). Following electrophoresis, proteins are transferred onto a polyvinylidene fluoride (PVDF) membrane, for western blot analysis using a relevant primary antibody. Detection of protein is accomplished by an enhanced chemiluminescent (ECL) detection method. The extent of tyrosine phosphorylation of HER2/erbB2 is measured by the LAS-1000 plus lumino-image analyser. The concentration of Mubritinib that inhibits HER2/erbB2 phosphorylation by 50% (IC50) is calculated from a dose–response curve generated by least-squares linear regression of the response using SAS software. |
细胞实验 | Several cancer cell lines (A549, lung adenocarcinoma epithelial cells; HeLa, cervical cancer cells; MDA-MB-231, breast cancer cells; HepG2, liver cancer cells) are treated with various concentrations (0-15 μM) of Az or compound 7 as a negative control for 18 hr. Cell viabilities are then determined using an MTT assay.(Only for Reference) |
别名 | Apoptosis Activator VII |
分子量 | 625.56 |
分子式 | C33H25F6N3O3 |
CAS No. | 1054543-47-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 24 mg/mL (38.4 mM)
DMSO: 93 mg/mL (148.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.5986 mL | 7.9928 mL | 15.9857 mL | 39.9642 mL |
5 mM | 0.3197 mL | 1.5986 mL | 3.1971 mL | 7.9928 mL | |
10 mM | 0.1599 mL | 0.7993 mL | 1.5986 mL | 3.9964 mL | |
20 mM | 0.0799 mL | 0.3996 mL | 0.7993 mL | 1.9982 mL | |
DMSO | 50 mM | 0.032 mL | 0.1599 mL | 0.3197 mL | 0.7993 mL |
100 mM | 0.016 mL | 0.0799 mL | 0.1599 mL | 0.3996 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Apoptozole 1054543-47-3 Apoptosis Cytoskeletal Signaling Metabolism HSP domain Heat shock proteins inhibit Inhibitor Apoptosis Activator VII Hsp70 ATPase Hsc70 inhibitor