ABT-751
作者：齐岳
发布时间：2023-09-14
08:56:52
点击数：
产品名称：ABT-751
产品描述：
| 产品描述 | ABT-751 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*的犬中,ABT-751限制剂量限制性毒性,包括呕吐、腹泻,厌食,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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 37.1 mg/mL (100 mM)
Ethanol: 9.3 mg/mL (25 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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