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141430-65-1

141430-65-1 structure
141430-65-1 structure
  • Name: ABT-751 (E7010)
  • Chemical Name: abt-751
  • CAS Number: 141430-65-1
  • Molecular Formula: C18H17N3O4S
  • Molecular Weight: 371.410
  • Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Hydroxypyridine
  • Create Date: 2018-12-31 08:30:36
  • Modify Date: 2025-08-22 16:58:12
  • 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.IC50 Value: 1.5 μM(neuroblastoma); 3.4 μM(non-neuroblastoma)Target: Microtubule/Tubulinin 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.

Name abt-751
Synonyms Tazac
Benzenesulfonamide, N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxy-
Galitidin
Distaxid
Zanizal
Calmaxid
N-{2-[(4-Hydroxyphenyl)amino]-3-pyridinyl}-4-methoxybenzenesulfonamide
nizatidine
Acinon
Nizax
Cronizat
Axid
E 7010
Description 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.IC50 Value: 1.5 μM(neuroblastoma); 3.4 μM(non-neuroblastoma)Target: Microtubule/Tubulinin 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.
Related Catalog
References

[1]. Huang SM et al.,Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling., Nature. 2009 Oct 1;461(7264):614-20.

[2]. Elizabeth Fox et al. A Phase I Study of ABT-751, an Orally Bioavailable Tubulin Inhibitor, Administered Daily for 21 Days Every 28 Days in Pediatric Patients with Solid Tumors Clin Cancer Res February 15, 2008 14; 1111

[3]. Aggarwal C, Somaiah N, Simon G.,Antiangiogenic agents in the management of non-small cell lung cancer: where do we stand now and where are we headed?,Cancer Biol Ther. 2012 Mar;13(5):247-63.

[4]. Silver M, Rusk A, Phillips B, Beck E, Jankowski M, Philibert J, Hahn K, Hershey E, McKeegan E, Bauch J, Krivoshik A, Khanna C.,Evaluation of the oral antimitotic agent (ABT-751) in dogs with lymphoma.,J Vet Intern Med. 2012 Mar-Apr;26(2):349-54. doi: 10.1111/j.1939-1676.2012.00892.x. Epub 2012 Feb 28.

[5]. Gaynon PS, Harned TM; for the Therapeutic Advances in Childhood LeukemiaLymphoma (TACL) Consortium.

Density 1.4±0.1 g/cm3
Boiling Point 551.0±60.0 °C at 760 mmHg
Melting Point 162 °C(dec.)
Molecular Formula C18H17N3O4S
Molecular Weight 371.410
Flash Point 287.0±32.9 °C
Exact Mass 371.093964
PSA 108.93000
LogP 4.58
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.677
RTECS DB2734000
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