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    ABT-751 (E 7010)
    ABT-751 (E 7010)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1607
    CAS #: 141430-65-1 Purity ≥98%

    Description: 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. ABT-751 binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules which block the G2/M phase of the cell cycle and promote apoptosis. It is not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin.  In endothelial cells, ABT-751 caused significant loss of microtubules and endothelial cell retraction within 1 h in a does-dependent and reversible way.

    References: Pediatr Blood Cancer. 2010 Jan;54(1):47-54; Cancer Chemother Pharmacol. 2007 May;59(6):725-32. 

    Related CAS#: 857447-92-8; 141450-48-8 (HCl); 141430-65-1 (free base)

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    Molecular Weight (MW)371.41
    FormulaC18H17N3O4S
    CAS No.141430-65-1 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (199.2 mM)
    Water:<1 mg/mL
    Ethanol: 12 mg/mL (32.3 mM)
    Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 15 mg/mL 
    SynonymsE7010; E 7010; E-7010; ABT751; ABT-751; ABT 751


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: 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. 


    Cell Assay: Cells (HOS, HTB-186 Daoy, TC-71, RD, SK-N-AS, SK-N-DZ, LD and KCNR cells), in 1640 RPMI media with FBS, are plated in triplicate onto 96 well tissue culture plates in numbers determined optimal for confluent monolayer growth (5,000 cells/well for HOS, HTB-186 Daoy; 10,000 cells/well for TC-71, RD, SK-N-AS, SK-N-DZ, LD; 30,000 cells/well for KCNR), with an automated, multichannel pipette system. Cells are incubated for 24 hours at 37 °C/5% CO2 then exposed to vehicle control (1.25% DMSO/H2O), VCR (0.1–1000 nM), ABT-751 (0.1 nM–100 μM), and in 4 cell lines (SK-N-AS, KCNR, RD, TC-71) combretastatin (0.1–1000 nM) for 72 hours. Cells are fixed with trichloroacetic acid (final concentration 10%) at 4 °C, washed, then dried at room temperature, stained with SRB in 1% acetic acid and dye is then solubilized with Tris base. Optical density measurements are performed at 540 and 405 nm dual wavelengths in a Bio-Tek EL 340 UV plate reader.

    In VivoIn this 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.
    Animal modelCalu-6 NSCLC, HT-29 colon, and HCT-116 cells are injected into athymic mice.
    Formulation & DosageDissolved in 4% ethanol/96% dextrose solution (D5W) with 1 eq. 1 N HCl; 75 or 100 mg/kg; P.O.
    ReferencesPediatr Blood Cancer. 2010 Jan;54(1):47-54; Cancer Chemother Pharmacol. 2007 May;59(6):725-32.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ABT-751

    Cell survival curves for 2 non-neuroblastoma (A. RD and B. TC-71) and 2 neuroblastoma (C. KCNR and D. SK-N-AS) cell lines exposed to a range of concentrations of ABT-751 or vincristine (VCR). Pediatr Blood Cancer. 2010 Jan;54(1):47-54.
     

    ABT-751

    Pediatr Blood Cancer. 2010 Jan;54(1):47-54.
     

    ABT-751

    Confocal microscopy of polymerized tubulin utilizing fluorescence labeled anti-acetylated ! tubulin antibody and of dynamic tubulin using anti-tyrosinated ! tubulin antibody at the IC90 concentrations of VCR, ABT-751, combretastatin and a vehicle control in KCNR cells. Pediatr Blood Cancer. 2010 Jan;54(1):47-54.


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