COMBRETASTATIN A1
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
- 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, 4?mg/kg |
| Administration: | I.v. every other day for 4 weeks |
| Result: | Resulted in a significant tumor volume reduction at the dose of 2?mg/kg or 4?mg/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
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COMBRETASTATIN A1(109971-63-3)Related Product Information
- Combretastatin A4 phosphate disodium salt
- COMBRETASTATIN A-4
- (Z)-3-Ethoxy-6-(3,4,5-Trimethoxystyryl)Benzene-1,2-Diol
- COMBRETASTATIN A1
- cis Resveratrol
- combretastatin A-2
- (R)-(-)-Combretastatin,COMBRETASTATIN
- Combretastatin D2
- combretastatin B-1
- Combretastatin D1
- Combretastatin A-3
- Combretastatin A-1 di-O-phosphate tetra-sodium salt
- (E)- Combretastatin A4
- combretastatin B-3
- combretastatin B-4
- combretastatin A5
- TETRASODIUM COMBRETASTATIN A1 2',3'-O-DIPHOSPHATE
- COMBRETASTATIN A4