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| | COMBRETASTATIN A1 Basic information |
| Product Name: | COMBRETASTATIN A1 | | Synonyms: | 3-methoxy-6-[(E)-2-(3,4,5-trimethoxyphenyl)ethenyl]benzene-1,2-diol;COMBRETASTATIN A1;(Z)-3,4,4',5-Tetramethoxy-2',3'-dihydroxystilbene;(Z)-3',4,4',5'-Tetramethoxystilbene-2,3-diol;3-Methoxy-6-[(Z)-3,4,5-trimethoxystyryl]-1,2-benzenediol;(Z)-3-Methoxy-6-(3,4,5-Trimethoxystyryl)Benzene-1,2-Diol;Combretastatin A1( 3-Methoxy-6-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-benzene-1,2-diol );1,2-Benzenediol, 3-methoxy-6-[(1Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]- | | CAS: | 109971-63-3 | | MF: | C18H20O6 | | MW: | 332.35 | | EINECS: | | | Product Categories: | Combretastatin | | Mol File: | 109971-63-3.mol |  |
| | COMBRETASTATIN A1 Chemical Properties |
| Melting point | 113-115 °C(Solv: chloroform (67-66-3); hexane (110-54-3)) | | Boiling point | 528.4±50.0 °C(Predicted) | | density | 1.251±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMF: 5 mg/ml; DMSO: 5 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 3 mg/ml | | form | A crystalline solid | | pka | 8.89±0.45(Predicted) | | color | White to off-white |
| | COMBRETASTATIN A1 Usage And Synthesis |
| Uses | Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects[1][2][3]. | | in vivo | Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume in HepG2 subcutaneous xenograft model[2].
Combretastatin A-1 (2 mg/kg; every other day for 21 days) shows enhanced apoptosis in orthotopic hepatocellular carcinoma mouse model[2]. | Animal Model: | Male athymic BALB/c nu/nu mice (16-18 g; 4-6 weeks old) were inoculated with HepG2 cells[2] | | Dosage: | 1, 2, 4mg/kg | | Administration: | I.v. every other day for 4 weeks | | Result: | Resulted in a significant tumor volume reduction at the dose of 2mg/kg or 4mg/kg. |
| | References | [1] Pettit GR, et, al. Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum. J Nat Prod. Jan-Feb 1987;50(1):119-31. DOI:10.1021/np50049a016
[2] Mao J, et, al. Combretastatin A-1 phosphate, a microtubule inhibitor, acts on both hepatocellular carcinoma cells and tumor-associated macrophages by inhibiting the Wnt/β-catenin pathway. Cancer Lett. 2016 Sep 28;380(1):134-43. DOI:10.1016/j.canlet.2016.06.020
[3] Holwell SE, et, al. Anti-tumor and anti-vascular effects of the novel tubulin-binding agent combretastatin A-1 phosphate. Anticancer Res. Nov-Dec 2002;22(6C):3933-40. PMID:12553015 |
| | COMBRETASTATIN A1 Preparation Products And Raw materials |
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