| 名稱(chēng) | ABT-751 |
| 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在HT-29結(jié)腸異種移植模型中,ABT-751也顯示出顯著的作為單一藥劑的抗腫瘤活性,并且在與5-FU聯(lián)用產(chǎn)生劑量依賴(lài)性的生長(zhǎng)延遲增強(qiáng). 在此Calu-6異種移植模型中,ABT-751作為100和75 mg/kg /天的單一藥劑顯示出顯著的抗腫瘤活性,而與順鉑組合時(shí),ABT-751顯示劑量依賴(lài)性的生長(zhǎng)延遲增強(qiáng).在患淋巴癌的犬中,ABT-751限制劑量限制性毒性,包括嘔吐、腹瀉,厭食,最大耐受劑量為350 mg/m(2) PO q24 h. |
| 體內(nèi)活性 | ABT-751顯示出對(duì)動(dòng)態(tài)微管的選擇性作用并且保留穩(wěn)定的微管,從而解釋了在ABT-751的IC90濃度下乙?；腿ダ野彼幡?微管蛋白陽(yáng)性聚合小管的持久性。在體外,ABT-751顯示選擇性細(xì)胞毒性,在神經(jīng)母細(xì)胞瘤中IC50為0.6-2.6 μM,在其他實(shí)體瘤細(xì)胞系中為0.7-4.6 μM。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 37.1 mg/mL (100 mM)
Ethanol : 9.3 mg/mL (25 mM)
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| 關(guān)鍵字 | ABT-751 | Microtubule/Tubulin | Autophagy | ABT 751 | Inhibitor | inhibit | ABT751 | E-7010 | E 7010 |
| 相關(guān)產(chǎn)品 | Oxyresveratrol | Guanidine hydrochloride | Naringin | Taurine | Gefitinib | Xylitol | Hydroxychloroquine | Curcumin | Stavudine | Myricetin | Paeonol | Sodium 4-phenylbutyrate |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 抗癌活性化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 抗衰老化合物庫(kù) | NO PAINS 化合物庫(kù) | 微管靶向化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù) |