Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ABT-751 (E7010) 是一种新型的生物相容性的微管蛋白结合剂,用于治疗肺癌、非小细胞肺癌和非小细胞肺癌。它是磺胺类抗有丝分裂抑制剂,对神经母细胞瘤细胞株和非神经母细胞瘤细胞株的IC50分别为1.5 和 3.4 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 187 | 现货 | ||
5 mg | ¥ 415 | 现货 | ||
10 mg | ¥ 629 | 现货 | ||
25 mg | ¥ 1,263 | 现货 | ||
50 mg | ¥ 1,854 | 现货 | ||
100 mg | ¥ 2,953 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 460 | 现货 |
产品描述 | ABT-751 (E7010) has been investigated for the treatment of Lung Cancer, Non-Small Cell Lung Cancer, and Non-Small-Cell Lung Cancer. |
靶点活性 | Neuroblastoma:1.5 μM |
体外活性 | 在HT-29结肠异种移植模型中,ABT-751也显示出显著的作为单一药剂的抗肿瘤活性,并且在与5-FU联用产生剂量依赖性的生长延迟增强. 在此Calu-6异种移植模型中,ABT-751作为100和75 mg/kg /天的单一药剂显示出显著的抗肿瘤活性,而与顺铂组合时,ABT-751显示剂量依赖性的生长延迟增强.在患淋巴癌的犬中,ABT-751限制剂量限制性毒性,包括呕吐、腹泻,厌食,最大耐受剂量为350 mg/m(2) PO q24 h. |
体内活性 | ABT-751显示出对动态微管的选择性作用并且保留稳定的微管,从而解释了在ABT-751的IC90浓度下乙酰化和去酪氨酸α-微管蛋白阳性聚合小管的持久性。在体外,ABT-751显示选择性细胞毒性,在神经母细胞瘤中IC50为0.6-2.6 μM,在其他实体瘤细胞系中为0.7-4.6 μM。 |
激酶实验 | High-throughput screening: For HTS, USP1-UAF1 activity is monitored using ubiquitin-rhodamine 110 as a substrate, where hydrolysis of the amide bond between the C-terminal glycine of ubiquitin and rhodamine results in an increase in fluorescence. The assay is miniaturized to a 4 μL volume in a 1,536-well format and is used to screen approximately 402,701 compounds in quantitative HTS mode, with each compound tested over a range of four to five concentrations. The assay shows robust performance with an average Z'factor of 0.8 throughout the screen. |
细胞实验 | Cells, in 1640 RPMI media with FBS, are plated in triplicate onto 96 well tissue culture plates in numbers determined optimal for confluent monolayer growth (5,000 cells/well for HOS, HTB-186 Daoy; 10,000 cells/well for TC-71, RD, SK-N-AS, SK-N-DZ, LD; 30,000 cells/well for KCNR), with an automated, multichannel pipette system. Cells are incubated for 24 hours at 37 °C/5% CO2 then exposed to vehicle control (1.25% DMSO/Water), VCR (0.1–1000 nM), ABT-751 (0.1 nM–100 μM), and in 4 cell lines (SK-N-AS, KCNR, RD, TC-71) combretastatin (0.1–1000 nM) for 72 hours. Cells are fixed with trichloroacetic acid (final concentration 10%) at 4 °C, washed, then dried at room temperature, stained with SRB in 1% acetic acid and dye is then solubilized with Tris base. Optical density measurements are performed at 540 and 405 nm dual wavelengths in a Bio-Tek EL 340 UV plate reader. (Only for Reference) |
别名 | E7010 |
分子量 | 371.41 |
分子式 | C18H17N3O4S |
CAS No. | 141430-65-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 37.1 mg/mL (100 mM)
Ethanol: 9.3 mg/mL (25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.6924 mL | 13.4622 mL | 26.9244 mL | 67.3111 mL |
5 mM | 0.5385 mL | 2.6924 mL | 5.3849 mL | 13.4622 mL | |
10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL | 6.7311 mL | |
20 mM | 0.1346 mL | 0.6731 mL | 1.3462 mL | 3.3656 mL | |
DMSO | 50 mM | 0.0538 mL | 0.2692 mL | 0.5385 mL | 1.3462 mL |
100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6731 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。
ABT-751 141430-65-1 Autophagy Cytoskeletal Signaling Microtubule Associated E7010 Microtubule/Tubulin ABT 751 Inhibitor inhibit ABT751 E-7010 E 7010 inhibitor