Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodiummicrotubule destabilizing drug, water-soluble CAS# 168555-66-6 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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. | ||
| 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.
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: | |||||
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Dilution Calculator
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Molarity Calculator
| 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. | |||||
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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.
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