ABT-751 (E7010)
Catalog No.S1165
Molecular Weight(MW): 371.41
ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.
Cited by 2 Publications
3 Customer Reviews
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Cell viability in H292 monolayer cells after 3-day treatment and spheroid volume in H292 3D culture after 7-day treatment with ABT751. Data points are means ?SD for three individual experiments. IC50 values were calculated to emphasize the differences in drug potency in 2D verses 3D cultures. ABT751, IC50 of 177.2 ?17.3 nM for 2D and 670.2 ?257.6 nM for 3D.
Bioorg Med Chem 2013 21, 922-31. ABT-751 (E7010) purchased from Selleck.
3D spheroid integrity following treatment with ABT751. Representative phase contrast imagines of H292 multi-cellular 3D spheroid at the onset of the treatment and after a 7-day treatment interval with various concentrations. Magnification: 10 X objective, scan bar: 200 μm. Dose and time dependent curves of ABT751 with 3D spheroid assay.
Bioorg Med Chem 2013 21, 922-31. ABT-751 (E7010) purchased from Selleck.
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Western blot analysiswas used to validate the regulation of β1-tubulin to vinculin. (A) Inhibited effects of ABT-751 on the β1-tubulin.Washed human plateletswere treatedwith 0, 2.5, 5, 10 and 20 μg/ml ABT-751 for 60 min then stimulated with 0.3 U thrombin (B) Protein expression of vinculin and Talin1 in washed platelets. The representative bands were from different gels for repeated experiments. After densitometric analysis, the values of proteins were normalized against GAPDH, respectively. Data are shown as the mean ± S.D. (n =3-4 per group). ##P < 0.01 vs normal group, **P < 0.01 vs thrombin group, ++P < 0.01 vs thrombin group.
Fitoterapia, 2017, 116:106-115. ABT-751 (E7010) purchased from Selleck.
Purity & Quality Control
Choose Selective Microtubule Associated Inhibitors
Biological Activity
| Description | ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | An orally bioavailable tubulin-binding and antimitotic sulfonamide. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
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. [1] |
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| Cell Data |
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| In vivo | In 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. [2] 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. [3] |
Protocol
| Cell Research:[1] |
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| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 74 mg/mL (199.24 mM) |
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| Ethanol | 12 mg/mL (32.3 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
15 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 371.41 |
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| Formula | C18H17N3O4S |
| CAS No. | 141430-65-1 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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