Home >> Research Area >>Cell Cycle/Checkpoint>>Microtubule/Tubulin>> Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

microtubule destabilizing drug, water-soluble CAS# 168555-66-6

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Catalog No. BCC4600----Order now to get a substantial discount!

Product Name & Size Price Stock
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 5mg $58 In Stock
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 10mg Please Inquire In Stock
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 20mg Please Inquire Please Inquire
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 50mg Please Inquire Please Inquire
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 100mg Please Inquire Please Inquire
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 200mg Please Inquire Please Inquire
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 500mg Please Inquire Please Inquire
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Number of papers citing our products

Chemical structure

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

3D structure

Chemical Properties of Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Cas No. 168555-66-6 SDF Download SDF
PubChem ID 6918309 Appearance Powder
Formula C18H19Na2O8P M.Wt 440.29
Type of Compound N/A Storage Desiccate at -20°C
Synonyms CA 4DP; CA 4P; Combretastatin A4 disodium phosphate
Solubility H2O : 4.5 mg/mL (10.22 mM; Need ultrasonic and warming)
DMF : < 1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
Chemical Name disodium;[2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl] phosphate
SMILES COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)OP(=O)([O-])[O-].[Na+].[Na+]
Standard InChIKey VXNQMUVMEIGUJW-XNOMRPDFSA-L
Standard InChI InChI=1S/C18H21O8P.2Na/c1-22-14-8-7-12(9-15(14)26-27(19,20)21)5-6-13-10-16(23-2)18(25-4)17(11-13)24-3;;/h5-11H,1-4H3,(H2,19,20,21);;/q;2*+1/p-2/b6-5-;;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

DescriptionFosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. IC50 Value: 4 nM [1] Target: microtubule in vitro: Cytotoxic IC(50) values of CA-4 in human bladder cancer cells were below 4 nM. 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 [1]. The enhanced apoptosis induced by dasatinib plus CA-4 was accompanied by a greater extent of mitochondrial depolarization, caspase-3 activation and PARP cleavage in HO-8910 cells. Furthermore, elevated expression of Mcl-1 led to a reduced apoptosis induced by dasatinib plus CA-4, highlighting that downregulated Mcl-1 was necessary for the potentiating effect of dasatinib to CA-4-triggered apoptosis [2]. in vivo: The increased anticancer efficacy of dasatinib combined with CA-4 was further validated in a human HO-8910 ovarian cancer xenograft model in nude mice [2]. There was a significant, concentration dependent increase in mean arterial blood pressure with a maximum increase of about 60% of the baseline MAP at 30 mg/kg of CA4P compared to the saline control. However, there was no significant increase in the cardiac troponin I level after CA4P injection [3]. Clinical trial: A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome [4].

References:
[1]. Shen CH, Shee JJ, Wu JY, Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model. Br J Pharmacol. 2010 Aug;160(8):2008-27. [2]. Zhang C, Zhou SS, Li XR, Enhanced antitumor activity by the combination of dasatinib and combretastatin A-4 in vitro and in vivo. Oncol Rep. 2013 Jun;29(6):2275-82. [3]. Ke Q, Bodyak N, Rigor DL, Pharmacological inhibition of the hypertensive response to combretastatin A-4 phosphate in rats. Vascul Pharmacol. 2009 Nov-Dec;51(5-6):337-43. [4]. Mooney CJ, Nagaiah G, Fu P, A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome. Thyroid. 2009 Mar;19(3):233-40.

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2712 mL 11.3562 mL 22.7123 mL 45.4246 mL 56.7808 mL
5 mM 0.4542 mL 2.2712 mL 4.5425 mL 9.0849 mL 11.3562 mL
10 mM 0.2271 mL 1.1356 mL 2.2712 mL 4.5425 mL 5.6781 mL
50 mM 0.0454 mL 0.2271 mL 0.4542 mL 0.9085 mL 1.1356 mL
100 mM 0.0227 mL 0.1136 mL 0.2271 mL 0.4542 mL 0.5678 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is a microtubule destabilizing drug, a water-soluble prodrug of combretasain A4(CA4) and a tumor vascular-targeting agent.

Microtubule is the cylindrical and filamentous structure that required for cell shape, migration, cilia and flagella mobility etc. Tubulin is the major component of microtubules

In proliferative endothelial cells, CA4P (dose less than 1/10 of the max. tolerated dose) leaded to tumor vascular shutdown, and short drug exposure of CA4P caused significant long-term anti-proliferative and cytotoxic effects. [1] In CA40 treated endothelia cell, myosin light chain was phosphorylated and lead to actinomyosin contractility, assembly of actin stress fibers and focal adhesions formation. [2] In HUVEC cells, CA4P blocked growth factor–induced endothelial cell proliferation and migration and impaired capillary tube formation. [3]

In C57BL/6 mice, CA4P treatment in combination with mAb against VE-cardherin facilitated B16 melanoma tumor necrosis and inhibited tumor neoangionesis. [3] In human breast cancer models in vivo, 6 hours after CA4P administration showed a 93% decreased functional vascular volume and lasted over the next 12 hours. [1]

References:
[1] Dark GG, Hill SA, Prise VE, Tozer GM, Pettit GR, Chaplin DJ.  Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature.  Cancer Res. 1997 May 15;57(10):1829-34.
[2] Kanthou C, Tozer GM.  The tumor vascular targeting agent combretastatin A-4-phosphate induces reorganization of the actin cytoskeleton and early membrane blebbing in human endothelial cells.  Blood. 2002 Mar 15;99(6):2060-9.
[3] Vincent L, Kermani P, Young LM, Cheng J, Zhang F, Shido K, Lam G, Bompais-Vincent H, Zhu Z, Hicklin DJ, Bohlen P, Chaplin DJ, May C, Rafii S.  Combretastatin A4 phosphate induces rapid regression of tumor neovessels and growth through interference with vascular endothelial-cadherin signaling.  J Clin Invest.  2005 Nov;115(11):2992-3006.

Featured Products
New Products
 

Description

Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

Keywords:

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium,168555-66-6,CA 4DP; CA 4P; Combretastatin A4 disodium phosphate,Natural Products,Microtubule/Tubulin, buy Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium , Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium supplier , purchase Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium , Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium cost , Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium manufacturer , order Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium , high purity Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: