ABT-751 (also known as E7010) is a novel, potent and orally bioavailable antimitotic sulfonamide agent/tubulin inhibitor with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.
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ABT-751. Purity: >98.0%(HPLC). Synonyms: N-[2-[(4-Hydroxyphenyl)amino] pyridin-3-yl]-4-methoxybenzenesulfonamide. Documents: SDS | Specifications
Microtubules are major structure of cells. They play an important role in cellular movement, intracellular transport, cell shape, cellular polarity, and the segr ABT-751 has been investigated for the treatment of Lung Cancer, Non-Small Cell Lung Cancer, and Non-Small-Cell Lung Cancer.
ABT-751, as a single agent, has antitumor activity against a series of xenograft models including non-small cell lung cancer (NSCLC) and colon cancer. The current studies were conducted to determine whether ABT-751 enhances antitumor activity of standard cytotoxic therapies currently in clinical use.
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It binds to the colchicine binding site on beta-tubulin and inhibits polymerization of microtubules.
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A phase 1 study was conducted to determine the maximum tolerated dose and toxicities of ABT-751 in patients with advanced myelodysplastic syndrome and relapsed or refractory acute leukemias.
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ABT-751 is an antimitotic agent, inhibits microtubule polymerization, binds to β-tubulin on the colchine site; blocks cell cycle at G2M phase and induces apoptosis.
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Hande The pharmacokinetics and safety of ABT-751, a novel, orally bioavailable sulfonamide antimitotic agent: results of a phase 1 study. Clin.Cancer Res. 2006 PMID: 16675578 Citations. Currently there are no citations for ABT 751. Product Datasheets. COA Certificate of
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ABT-751 WDT5V5OB9F Investigational Source: NCT00436852: Phase 2 Interventional Completed Disseminated Neuroblastoma (2007 ABT-751 is an orally bioavailable tubulin-binding agent that is currently under clinical development for cancer treatment. In preclinical studies, ABT-751 showed antitumor activity against a broad spectrum of tumor lines including those resistant to conventional chemotherapies. ABT 751 is an inhibitor of microtubule polymerization that binds β-Tubulin on the colchine site. ABT 751 has been shown to block the cell cycle at G 2 M phase and induce apoptosis. Reproted to exhibit antitumor activity. Furthermore ABT 751 displays activity in cell lines resistant to vincristine, doxorubicin and cisplatin. References.
NCT00436852: Phase 2 Interventional Completed Disseminated Neuroblastoma (2007) ABT‐751 is a novel orally available antimitotic agent that binds to the colchicine site on beta tubulin and inhibits polymerization of microtubules. 1 ABT‐751 functions as a potent antimitotic agent by inhibiting the proliferation of a broad spectrum of human cancer cell lines at nanomolar to low micromolar concentrations in vitro (molecular weight, 371.4). 1, 2 Antimitotic agents fall Conclusions: ABT-751 associated toxicity was acceptable. The median time to progression and overall survival as demonstrated for ABT-751 were comparable to other agents considered active in this patient population and to current treatments approved for second … ABT-751 also induced early autophagy via upregulation of nuclear TP53 and downregulation of the AKT serine/threonine kinase (AKT)/mechanistic target of rapamycin (MTOR) pathway.