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ABT-751 (E7010)

Catalog No.GC15875

ABT-751 (E7010)(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.

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ABT-751 (E7010) Chemical Structure

Cas No.: 141430-65-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$61.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

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.

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.

Chemical Properties

Cas No. 141430-65-1 SDF
Chemical Name 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
Formula C18H17N3O4S M.Wt 371.41
Solubility ≥ 18.55 mg/mL in DMSO, ≥ 25.53 mg/mL in EtOH with ultrasonic Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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