化合物ABT-751 T1758

Product Introduction
Bioactivity


英文名: ABT-751

描述: 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。

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)

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.

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 37.1 mg/mL (100 mM)
Ethanol : 9.3 mg/mL (25 mM)


关键字: ABT-751 | Microtubule/Tubulin | Autophagy | ABT 751 | Inhibitor | inhibit | ABT751 | E-7010 | E 7010

相关产品: Tubulin inhibitor 1 | Indibulin | 4'-Demethylepipodophyllotoxin | TAI-1 | Rosabulin | 10-Deacetyl-7-xylosyl paclitaxel | McMMAF | TTBK1-IN-2 | Erbulozole | 7-epi-Taxol

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Microtubule-Targeted Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Autophagy Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途