DC Chemicals · Product datasheet

ABT-751(E 7010) — Datasheet

CAT. NO. DC7353

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ParameterValue
Chemical NameABT-751
CAS No.141430-65-1
SynonymsBenzenesulfonamide,N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxy-;ABT-751 (E7010);ABT-751;ABT 751;Acinon;Axid;Calmaxid;Cronizat;Distaxid;E7010;E-7010;Galitidin;nizatidine;Nizax;Tazac;Zanizal;N-[2-[(4-Hydroxyphenyl)amino]pyridin-3-yl]-4-methoxybenzenesulfonamide;ABT751;E 7010;WDT5V5OB9F;N-[2-[(4-HYDROXYPHENYL)AMINO]-3-PYRIDYL]-4-METHOXYBENZENESULFONAMIDE;N-(2-((4-Hydroxyphenyl)amino)-3-pyridinyl)-4-methoxybenzenesulfonamide;N-{2-[(4-hydroxyphenyl)amino]pyridin-3-yl}-4-methoxybenzenesulfonamide;N-(2-(4-hydroxyphenylamino)pyridin-3-yl)-4-methoxybenzenesulfonamide;N-[2-(4-hydroxyanilino)pyridin-3-yl]-
FormulaC18H17N3O4S
M.Wt371.41
SMILESS(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])(N([H])C1C([H])=C([H])C([H])=NC=1N([H])C1C([H])=C([H])C(=C([H])C=1[H])O[H])(=O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

ABT-751(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.

In Vitro

ABT-751 shows 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. Furthermore, ABT-751 also exhibits a selective effect on dynamic microtubules and spares stable microtubules, accounting for the persistence of acetylated and detyrosinated α-tubulin positive polymerized tubules at the IC90 concentration of ABT-751.

In Vivo

In Calu-6 xenograft model, ABT-751 as a single agent at 100 and 75 mg/kg/day shows significant antitumor activity, while in combination with cisplatin, ABT-751 shows a dose-dependent enhancement in growth delay. In the HT-29 colon xenograft model, ABT-751 also shows significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay In combination with 5-FU. In dogs with lymphoma, ABT-751 exhibits the dose-limiting toxicities that included vomiting, diarrhea, anorexia, or some combination of these with a maximum tolerated dose (MTD) of 350 mg/m2 PO q24h. Furthermore, the mean AUC and Cmax for ABT-751 at the MTD of 350 mg/m2 is 5.55 μg-hour/mL and 0.9 μg/mL, respectively.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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