ABT-751 is an orally bioavailable tubulin inhibitor with IC50 of about 1.5 and 3.4 µM in neuroblastoma and non-neuroblastoma cell lines, respectively. ABT-751 had a broad spectrum of antitumor activity in a panel of 30 tumor cell lines in vitro and in xenograft models of human tumors in vivo, including gastric, colorectal, lung, and breast cancer models. ABT-751 showed antitumor activity against a broad spectrum of tumor lines including those resistant to conventional chemotherapies. A single dose of ABT-751 (30 mg/kg, intravenously) induced a rapid, transient reduction in tumor perfusion. After 1 h, tumor perfusion decreased by 57% before recovering to near pretreatment levels within 6 h. In contrast, ABT-751 produced little change in muscle perfusion at either time point. ABT-751, at concentrations corresponding to plasma levels achieved in vivo, caused endothelial cell retraction and significant loss of microtubules within 1 h.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥72 mg/mL|
ABT-751 in Relapsed Childhood Acute Lymphoblastic Leukemia.
Gaynon et al. J Pediatr Hematol Oncol. 2012 May 10. PMID: 22584778.
Evaluation of the oral antimitotic agent (ABT-751) in dogs with lymphoma.
Silver et al. J Vet Intern Med. 2012 Mar-Apr;26(2):349-54. PMID: 22369215.
Phase I/II study of pemetrexed with or without ABT-751 in advanced or metastatic non-small-cell lung cancer.
Rudin et al. J Clin Oncol. 2011 Mar 10;29(8):1075-82. PMID: 21300929.
Pharmacokinetics of orally administered ABT-751 in children with neuroblastoma and other solid tumors.
Fox et al. Cancer Chemother Pharmacol. 2010 Sep;66(4):737-43. PMID: 20044751.
Clinical outcome in children with recurrent neuroblastoma treated with ABT-751 and effect of ABT-751 on proliferation of neuroblastoma cell lines and on tubulin polymerization in vitro.
Meany et al. Pediatr Blood Cancer. 2010 Jan;54(1):47-54. PMID: 19731320.
|Related Microtubule Products|
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VcMMAE is a anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
Crolibulin (also known as EPC2407 and crinobulin) is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
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