ABT-751

ABT-751 (E7010) 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 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer[1][2][3][4][5][6][7][8].

Product Specifications

CAS Number

[141430-65-1]

Product Name Alternative

E7010

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; Microtubule/Tubulin

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage; Cytoskeleton

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ABT-751.html

Purity

99.40

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

COC1=CC=C(C=C1)S(=O)(NC2=C(N=CC=C2)NC3=CC=C(C=C3)O)=O

Molecular Formula

C18H17N3O4S

Molecular Weight

371.41

Precautions

H302, H315, H319, H335

References & Citations

[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, 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.|[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.|[6]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.|[7]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.|[8]Morton CL, et al. Evaluation of ABT-751 against childhood cancer models in vivo. Invest New Drugs. 2007;25 (4) :285-295.