141450-48-8
Chemical Structure
ABT-751 hydrochloride
Synonym(s): E7010 hydrochloride
- CAS No.: 141450-48-8
- Formula:C18H18ClN3O4S
- Molecular Weight:407.87
IUPAC Name: N-(2-((4-hydroxyphenyl)amino)pyridin-3-yl)-4-methoxybenzenesulfonamide hydrochloride
InChIKey: KWQWWUXRGIIBAS-UHFFFAOYSA-N
SMILES: COC1=CC=C(C=C1)S(=O)(NC2=C(N=CC=C2)NC3=CC=C(C=C3)O)=O.[H]Cl
Biological Activity: ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer[1][2][3][4][5][6][7][8][9].
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ABT-751 hydrochloride | ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer. | |||||||||||||||||||||
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- [1]. Huang SM et al.,Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling., Nature. 2009 Oct 1;461(7264):614-20. [Content Brief]
- [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, et al. 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. [Content Brief]
- [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. [Content Brief]
- [5]. Gaynon PS, Harned TM; for the Therapeutic Advances in Childhood LeukemiaLymphoma (TACL) Consortium. [Content Brief]
- [6]. Yoshimatsu K, et al. Mechanism of action of E7010, an orally active sulfonamide antitumor agent: inhibition of mitosis by binding to the colchicine site of tubulin. Cancer Res. 1997;57(15):3208-3213. [Content Brief]
- [7]. Morton CL, et al. Evaluation of ABT-751 against childhood cancer models in vivo. Invest New Drugs. 2007;25(4):285-295. [Content Brief]
- [8]. David Frost, et al. ABT-751, an oral antimitotic, shows additive and synergistic activity with docetaxel in preclinical models. Cancer Res 1 May 2007; 67 (9_Supplement): 1426.
Keywords
