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Fosbretabulin Disodium

Catalog No. T6272 CAS 168555-66-6

Synonyms: Combretastatin A4 Phosphate, CA 4DP, CA 4P, Combretastatin A4 disodium phosphate, Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

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Fosbretabulin Disodium Chemical Structure

Fosbretabulin Disodium, CAS 168555-66-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 173.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 369.00

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Purity: 99.96%

Purity: 99.83%

Purity: 97.43%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.
Targets&IC50	Tubulin: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]
Kinase Assay	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	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)

Synonyms	Combretastatin A4 Phosphate, CA 4DP, CA 4P, Combretastatin A4 disodium phosphate, Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
Molecular Weight	440.29
Formula	C18H19O8P·2Na
CAS No.	168555-66-6

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 10 mM

DMSO: Insoluble

References and Literature

1. Woods JA, et al. Br J Cancer 1995, 71(4), 705-711. 2. Dark GG, et al. Cancer Res 1997, 57(10), 1829-1834. 3. Kathou C, et al. Blood, 2002, 99(6), 2060-2069. 4. Vincent L, et al. J Clin Invest, 2005, 115(11), 21992-32006. 5. Tozer GM, et al. Cancer Res, 1999, 59(7), 1626-1634.

Citations

1. Han T, Duan Q, Yang R, et al. Monitoring the therapeutic efficacy of CA4P in the rabbit VX2 liver tumor using dynamic contrast-enhanced MRI. Diagnostic and Interventional Radiology. 2021, 27(5): 587. 2. Meng F, Zou B, Yang R, et al. The diagnostic efficiency of the perfusion-related parameters in assessing the vascular disrupting agent (CA4P) response in a rabbit VX2 liver tumor model. Acta Radiologica. 2021: 02841851211032450.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Microtubule-Targeted Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library NO PAINS Compound Library Natural Product Library

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Keywords

Fosbretabulin Disodium 168555-66-6 Apoptosis Cytoskeletal Signaling Microtubule Associated Microtubule/Tubulin Combretastatin A4 Phosphate tumour endothelia CA 4DP CA 4P Combretastatin A4 disodium phosphate tubulin Combretastatin A4 disodium Phosphate Combretastatin A4 disodium inhibit Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium neovessels destabilizing Inhibitor Fosbretabulin nascent inhibitor

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