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ABT-751 (E7010)

现货
Catalog No.
A1493
微管聚合抑制剂,抗有丝分裂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
10mg
¥ 850.00
现货
50mg
¥ 3,300.00
现货
100mg
¥ 4,700.00
现货

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Background

ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic agent [1][2].
Microtubules are major structure of cells. They play an important role in cellular movement, intracellular transport, cell shape, cellular polarity, and the segregation of chromosomes during mitosis[1].
ABT-751 binds to the colchicine site on ß-tubulin and inhibits polymerization of microtubules, which block the G2/M phase of the cell cycle and promote apoptosis [1]. In endothelial cells, ABT-751 caused significant loss of microtubules and endothelial cell retraction within 1 h in a does-dependent and reversible way [2].
In a rat subcutaneous tumor model, ABT-751 (30 mg/kg, intravenously) reduced tumor perfusion in a rapid, transient way. And tumor perfusion decreased by 57% after 1 h [3]. In Calu-6 xenograft model, ABT-751 dosed at 100 and 75 mg/kg/day showed significant antitumor activity. In combination with cisplatin, ABT-751 enhanced the growth delay in a dose-dependent way [1].
References:
[1]. Jorgensen TJ, Tian H, Joseph IB, et al. Chemosensitization and radiosensitization of human lung and colon cancers by antimitotic agent, ABT-751, in athymic murine xenograft models of subcutaneous tumor growth. Cancer Chemother Pharmacol, 2007, 59(6): 725-732.
[2]. Luo Y, Hradil VP, Frost DJ, et al. ABT-751, a novel tubulin-binding agent, decreases tumor perfusion and disrupts tumor vasculature. Anticancer Drugs, 2009, 20(6): 483-492.

文献引用

1.Jost M, Chen Y, et al. "Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent." Mol Cell. 2017 Oct 5;68(1):210-223.e6. PMID:28985505

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt371.41
Cas No.141430-65-1
FormulaC18H17N3O4S
Solubility≥18.55 mg/mL in DMSO, ≥25.53 mg/mL in EtOH with ultrasonic, <1.95 mg/mL in H2O
Chemical NameN-[2-(4-hydroxyanilino)pyridin-3-yl]-4-methoxybenzenesulfonamide
SDFDownload SDF
Canonical SMILESCOC1=CC=C(C=C1)S(=O)(=O)NC2=C(N=CC=C2)NC3=CC=C(C=C3)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

RD、TC-71、LD、HTB-186、HOS、SK-N-AS、SK-N-DZ和KCNR小儿实体瘤细胞系

溶解方法

该化合物在DMSO中的溶解度大于18.6 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

0.1 nM-100 μM

应用

ABT-751显示出选择性细胞毒性,在神经母细胞瘤中的IC50为0.6-2.6 μM,在其他实体瘤细胞系中的IC50值为0.7-4.6 μM。ABT-751对动态微管和保持稳定的微管表现出选择性作用,在IC90浓度下,ABT-751对乙酰化和去乙酰化α-微管蛋白阳性聚合小管具有持久性。

动物实验 [2]:

动物模型

携带Calu-6非小细胞肺癌(NSCLC)、HT-29结肠癌和HCT-116结肠癌异种移植物的裸鼠

给药剂量

每天口服一次,每次75或100 mg/kg/day,给药5天、休息5天,持续两个周期

应用

在Calu-6异种移植模型中,作为单一试剂,ABT-751在100和75 mg/kg/day显示出显著的抗肿瘤活性,ABT-751与顺铂组合使用,以剂量依赖性方式增强生长延迟。在HT-29结肠癌异种移植模型中,ABT-751作为单一药物显示出显著的抗肿瘤活性,并且与5-FU组合以剂量依赖性方式增强生长延迟。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Meany H J, Sackett D L, Maris J M, et al. Clinical outcome in children with recurrent neuroblastoma treated with ABT‐751 and effect of ABT‐751 on proliferation of neuroblastoma cell lines and on tubulin polymerization in vitro[J]. Pediatric blood & cancer, 2010, 54(1): 47-54.

[2]. Jorgensen T J, Tian H, Joseph I B J K, et al. Chemosensitization and radiosensitization of human lung and colon cancers by antimitotic agent, ABT-751, in athymic murine xenograft models of subcutaneous tumor growth[J]. Cancer chemotherapy and pharmacology, 2007, 59(6): 725-732.

生物活性

Description ABT-751是微管聚合的抑制剂。
靶点 microtubule polymerization          
IC50            

质量控制

化学结构

ABT-751 (E7010)

相关生物数据

ABT-751 (E7010)