Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Catalog No.S7204

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Chemical Structure

Molecular Weight(MW): 440.29

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Phase 3.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Phase 3.
Features A microtubule associated inhibitor with higher affinity to β-tubulin vs. Colchicine. Best for advanced solid tumors, anaplastic thyroid cancer, & choroidal neovascularization.
Targets
Tubulin [1]
(Cell-free assay)
2.4 μM
In vitro

Fosbretabulin disodium (Combretastatin A-4 phosphate disodium, CA4P disodium) is the water-soluble prodrug of combretastatin A4 (CA4), which is originally isolated from African tree Combretum caffrum. CA4 is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 μM), inhibits tubulin assembly with IC50 of 2.4 μM. [1] CA4 is cytotoxic towards proliferating but not quiescent endothelial cells, has potent and selective toxicity towards tumor vasculature. [2] CA4P (1 mM, 30 minutes) disrupts the endothelial microtubule cytoskeleton and mediates changes in endothelial cell morphology. CA4P stimulates actin stress fiber formation and membrane blebbing and increases monolayer permeability via Rho/Rho-kinase. [3] CA4P 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. [4]

In vivo CA4P causes rapid, extensive and irreversible vascular shutdown in experimental tumor models following the administration of a single dose at 10% of the maximum tolerated dose (MTD). CA4P causes a 93% reduction in vascular volume 6 h following drug administration. [2] CA4P(100 mg/kg, 6 h following administration) reduces tumor blood by approximately 100-fold, compared with approximately 7-fold in the spleen. [5]

Protocol

Kinase Assay:

[1]

+ Expand

Tubulin assembly-disassembly:

The assembly of microtubules from isolated tubulin is carried out spectrophotometrically at 350 nm and utilises the increase in turbidity which is associated with microtubule formation. Assembly is initiated by temperature increase from 10 to 35 °C. The effect of drugs on the increase in light absorption is carried. Drugs are dissolved in DMSO (<4%), which does not affect control assembly
Cell Research:

[4]

+ Expand
  • Cell lines: HUVECs
  • Concentrations: ~50 nM
  • Incubation Time: 12-48 h
  • Method:

    For the proliferation assay, the minimal concentration of FBS (1%) diluted in X-VIVO medium is used to allow sufficient viability of endothelial cells. After detachment, the cells are seeded at a concentration of 2×104 HUVECs in each well of 24-well plates, allowed to adhere overnight, and then incubated with or without cytokines (5 ng/ml FGF-2 or 5 ng/ml VEGF-A). CA4P is added at 0 – 50 nM. After incubation for 12, 24, 36, and 48 hours, cells are detached by trypsin/EDTA and manually counted using trypan blue exclusion.


    (Only for Reference)
Animal Research:

[5]

+ Expand
  • Animal Models: BD9 rats implanted with tumor
  • Formulation: 0.9% saline with a few drops of 5% Na2CO3
  • Dosages: 100 mg/kg, 3 ml/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 28 mg/mL (63.59 mM)
DMSO <1 mg/mL
Ethanol <1 mg/mL
In vivo Saline with a few drops of 5% Na2CO3 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.29
Formula

C18H19O8P.2Na

CAS No. 168555-66-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03014297 Not yet recruiting Neuroendocrine Tumors|Everolimus Lowell Anthony|University of Kentucky January 2017 Phase 1
NCT02641639 Recruiting Platinum Resistant Ovarian Cancer Mateon Therapeutics June 2016 Phase 2|Phase 3
NCT01701349 Withdrawn Anaplastic Thyroid Cancer Mateon Therapeutics March 2015 Phase 3
NCT02279602 Completed Neuroendocrine Tumors Mateon Therapeutics December 2014 Phase 2
NCT02055690 Recruiting Ovarian Neoplasms|Neoplasms, Ovarian|Ovarian Cancer Heather Driscoll|Novartis|Mateon Therapeutics|East and North Hertfordshire NHS Trust|The Christie NHS Foundation Trust September 2014 Phase 1|Phase 2
NCT02132468 Completed Neuroendocrine Tumors Mateon Therapeutics September 2014 Phase 2

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Microtubule Associated Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID