ABT-751 (E7010)

ABT-751 (E7010)

Catalog Number:
L002368311APE
Mfr. No.:
APE-A1493
Price:
$276
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      • Overview
        • Please contact us at for specific academic pricing.

          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].

          [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.

      • Properties
        • Alternative Name
          N-[2-(4-hydroxyanilino)pyridin-3-yl]-4-methoxybenzenesulfonamide
          CAS Number
          141430-65-1
          Molecular Formula
          C18H17N3O4S
          Molecular Weight
          371.41
          Appearance
          A solid
          Purity
          99.31%
          Solubility
          insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥25.53 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 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

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