Combretastatin A-1

Modify Date: 2024-01-02 10:35:31

Combretastatin A-1 structure	Common Name	Combretastatin A-1
	CAS Number	109971-63-3	Molecular Weight	332.348
	Density	1.3±0.1 g/cm3	Boiling Point	528.4±50.0 °C at 760 mmHg
	Molecular Formula	C₁₈H₂₀O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	273.3±30.1 °C

Use of Combretastatin A-1

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].

Name	combretastatin a1
Synonym	More Synonyms

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin
Target	Microtubule/Tubulin[1]
In Vitro	Combretastatin A-1 (72 h) inhibits the growth of various tumor cell lines in vitro, including HepG2, SMMC-7721, Hepa 1-6, LM-3, Bel-7402, Huh7, BGC-803, MDA-MB-231, MCF-7, A375, NCI-1975, CT-26, HT-29, A549 cells (IC50=9.2, 12.8, 32.9, 33.8, 38.4, 728.2, 12.2, 17.6, 46.0, 61.0, 256.3, 1075.0, 2082.0, 2247.0 nM, respectively)[2]. Combretastatin A-1 (1-10 nM; 24 h) induces apoptosis by microtubule depolymerization-induced AKT inactivation and the removal of GSK-3β inhibition in HepG2 cells[2]. Combretastatin A-1 (1-50 nM; 6 h) decreases the mitochondrial membrane potential (MMP) of HepG2 cells. Combretastatin A-1 shows dose-dependently ROS accumulation in HepG2 cells[2]. Western Blot Analysis[2] Cell Line: HepG2 cells Concentration: 1, 5, 10 nM Incubation Time: 24 hours Result: Significantly decreased Mcl-1 expression, but the Bcl-2 level was unchanged. Reduced p-GSK 3β (Ser9) without altering total GSK-3β protein levels, indicating an activation of GSK-3β. Reduced AKT phosphorylation on Ser473 without an obvious change in the total AKT protein levels.
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. [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. [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.

Density	1.3±0.1 g/cm3
Boiling Point	528.4±50.0 °C at 760 mmHg
Molecular Formula	C₁₈H₂₀O₆
Molecular Weight	332.348
Flash Point	273.3±30.1 °C
Exact Mass	332.125977
PSA	77.38000
LogP	3.84
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.627

Hazard Codes	Xi
HS Code	2909499000

HS Code	2909499000
Summary	2909499000. ether-alcohols and their halogenated, sulphonated, nitrated or nitrosated derivatives. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:5.5%. General tariff:30.0%

combretastatin A1 Z

Combretastatin A-1

3-methoxy-6-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]benzene-1,2-diol

(Z)-3',4,4',5'-Tetramethoxystilbene-2,3-diol

(Z)-3,4,4',5-Tetramethoxy-2',3'-dihydroxystilbene

Combretastatin A1( 3-Methoxy-6-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-benzene-1,2-diol )

(Z)-3-Methoxy-6-(3,4,5-Trimethoxystyryl)Benzene-1,2-Diol

1,2-Benzenediol, 3-methoxy-6-(2-(3,4,5-trimethoxyphenyl)ethenyl)-, (Z)-

(Z)-1-[3',4',5'-trimethoxyphenyl]-2-[2'',3''-dihydroxy-4''-methoxyphenyl]ethene

3-Methoxy-6-[(Z)-2-(3,4,5-trimethoxyphenyl)vinyl]-1,2-benzenediol

combretastatin A-2

1,2-Benzenediol, 3-methoxy-6-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]-

3-Methoxy-6-[(Z)-3,4,5-trimethoxystyryl]-1,2-benzenediol

3-Methoxy-6-[(Z)-2-(3,4,5-trimethoxyphenyl)vinyl]benzene-1,2-diol

DC Chemicals Limited
China
Product Name: Combretastatin A-1
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: COMBRETASTATIN A1
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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