Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Combretastatin A4 Phosphate Disodium (also called CA4P, Fosbretabulin; CA 4DP; CA-4P; Zybrestat) is the water-soluble prodrug that has to be activated to the active form, Combretastatin A4 (CA4), which is a highly potent MTA (microtubule-targeting agent) or tubulin inhibitor that acts as a potent anticancer agent that binds β-tubulin with a Kd of 0.4 μM in a cell-free assay. It was originally isolated from African tree Combretum caffrum. Combretastatin A4 inhibits the polymerization of tubulin with an IC50 of 2.4 μM, and also disrupts tumor vasculature. Under in vivo conditions, the prodrug fosbretabulin is dephosphorylated and activated to its active form, combretastatin A4, which binds to tubulin dimers and prevents microtubule polymerization, resulting in mitotic arrest and apoptosis in endothelial cells.
ln Vitro |
FosbretabuLin disodium suppresses the proliferation of leukemia P-388, pancreatic BXPC-3, neuroblast SK-N-SH, thyroid SW1736, lung-NSC NCI-H460, prostate DU-145, and pharyngeal FADU with EC50 of 0.0029, 0.23, and 0.00025, respectively., 0.00061, 0.00035, 0.00072, and 0.00045 μg/mL[2].
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ln Vivo |
In rats, fosbretabuLin disodium (100 mg/kg; ip) decreases tumor blood flow and raises mean arterial blood pressure (MABP) one and six hours after injection [3].
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Animal Protocol |
Animal/Disease Models: Male BD9 rats (7-9 weeks) bearing the sc implanted P22 tumor[3]
Doses: 100 mg/kg Route of Administration: A single ip injections Experimental Results: Dramatically raised the MABP by about 30%, and decreased the heart rate at 1 h after administration. decreased the blood flow in the tumor. |
References |
[1]. Shen CH, et, al. 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]. Pettit GR, et, al. Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41. J Med Chem. 2005 Jun 16;48(12):4087-99. [3]. Tozer GM, et, al. Combretastatin A-4 phosphate as a tumor vascular-targeting agent: early effects in tumors and normal tissues. Cancer Res. 1999 Apr 1;59(7):1626-34. |
Molecular Formula |
C18H19O8P.2NA
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Molecular Weight |
440.29
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CAS # |
168555-66-6
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Related CAS # |
168555-66-6 (disodium);222030-63-9 (free acid);404886-32-4 ( tromethamine);
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SMILES |
P(=O)(O[H])(O[H])OC1=C(C([H])=C([H])C(=C1[H])/C(/[H])=C(/[H])\C1C([H])=C(C(=C(C=1[H])OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H].[Na] |^1:48|
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 14.29 mg/mL (32.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: Saline with a few drops of 5% Na2CO3: 30 mg/mL  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2712 mL | 11.3562 mL | 22.7123 mL | |
5 mM | 0.4542 mL | 2.2712 mL | 4.5425 mL | |
10 mM | 0.2271 mL | 1.1356 mL | 2.2712 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.