ABT-751

• Description:

  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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• CAS Number:

  141430-65-1