Fosbretabulin disodium (Combretastatin A-4 phosphate) is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM. Fosbretabulin disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and it also disrupts tumor vasculature. Analyses of cell-cycle distribution showed CA-4 obviously induced G(2)-M phase arrest with sub-G(1) formation. The analyses of apoptosis showed that CA-4 induced caspase-3 activation and decreased BubR1 and Bub3 in cancer cells. Fosbretabulin disodium increases endothelial cell permeability, while inhibiting endothelial cell migration and capillary tube formation predominantly through disruption of VE-cadherin/β-catenin/Akt signaling pathway, thereby leading to rapid vascular collapse and tumor necrosis. Combretastatin A-4 phosphate (fosbretabulin disodium) is a microtubule destabilizing drug, a type of vascular-targeting agent, a compound designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.
|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||Water 25 mg/mL|
Enhanced antitumor activity by the combination of dasatinib and combretastatin A-4 in vitro and in vivo.
Zhang C, et al. Oncol Rep. 2013 Jun;29(6):2275-82. PMID: 23588374.
Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model.
Shen CH, et al. Br J Pharmacol. 2010 Aug;160(8):2008-27. PMID: 20649598.
A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome.
Mooney CJ, et al. Thyroid. 2009 Mar;19(3):233-40. PMID: 19265494.
|Related Microtubule Products|
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.
Epothilone D is a potent microtubule stabilizer.
|Estramustine phosphate sodium
Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
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