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ABT-751 (E7010) Sale

(Synonyms: N-[2-[(4-羟基苯基)氨基]-3-吡啶基]-4-甲氧基苯磺酰胺,E7010) 目录号 : GC15875

An inhibitor of microtubule polymerization

ABT-751 (E7010) Chemical Structure

Cas No.:141430-65-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥612.00
现货
10mg
¥599.00
现货
50mg
¥1,980.00
现货
100mg
¥3,150.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

RD, TC-71, LD, HTB-186, HOS, SK-N-AS, SK-N-DZ and KCNR pediatric solid tumor cell lines

Preparation method

The solubility of this compound in DMSO is > 18.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1 nM-100 μM

Applications

ABT-751 showed the selective cytotoxicity with IC50 of 0.6–2.6 μM in neuroblastoma and 0.7–4.6 μM in other solid tumor cell lines. ABT-751 exhibited a selective effect on dynamic microtubules and spared stable microtubules, accounting for the persistence of acetylated and detyrosinated α-tubulin positive polymerized tubules at the IC90 concentration of ABT-751.

Animal experiment [2]:

Animal models

Nude mice bearing Calu-6 non-small cell lung carcinoma (NSCLC), HT-29 colon carcinoma, and HCT-116 colon carcinoma xenografts

Dosage form

Orally once a day at 75 or 100 mg/kg/day on a 5-days-on, 5-days-off schedule for two cycles

Application

In the Calu-6 xenograft model, ABT-751 as a single agent at 100 and 75 mg/kg/day showed significant antitumor activity, while in combination with cisplatin, ABT-751 dose-dependently enhanced growth delay. In the HT-29 colon xenograft model, ABT-751 showed significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay in combination with 5-FU.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品描述

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.

Chemical Properties

Cas No. 141430-65-1 SDF
别名 N-[2-[(4-羟基苯基)氨基]-3-吡啶基]-4-甲氧基苯磺酰胺,E7010
化学名 N-[2-(4-hydroxyanilino)pyridin-3-yl]-4-methoxybenzenesulfonamide
Canonical SMILES COC1=CC=C(C=C1)S(=O)(=O)NC2=C(N=CC=C2)NC3=CC=C(C=C3)O
分子式 C18H17N3O4S 分子量 371.41
溶解度 ≥ 18.55 mg/mL in DMSO, ≥ 25.53 mg/mL in EtOH with ultrasonic 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6924 mL 13.4622 mL 26.9244 mL
5 mM 0.5385 mL 2.6924 mL 5.3849 mL
10 mM 0.2692 mL 1.3462 mL 2.6924 mL
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