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Fosbretabulin disodium

Cat. No. M2274
Fosbretabulin disodium Structure
Synonym:

Combretastatin A-4 phosphate, CA4P

Size Price Availability Quantity
10mg USD 125 In stock
25mg USD 220 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 440.29
Formula C18H19Na2O8P
CAS Number 168555-66-6
Purity >99%
Solubility Water 25 mg/mL
Storage at -20°C
References

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.

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Keywords: Fosbretabulin disodium, Combretastatin A-4 phosphate, CA4P supplier, Microtubule, inhibitors

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