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Combretastatin A-1

Catalog No. T36848 CAS 109971-63-3

Synonyms: Combretastatin A1

Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.

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Combretastatin A-1, CAS 109971-63-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 49.00
2 mg	5 days	$ 71.00
5 mg	In stock	$ 199.00

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Purity: 97.49%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.
Targets&IC50	A375:61 nM, LM-3:33.8 nM, HepG2 cells:9.2 nM, MCF-7 cells:46.0 nM, CT-26:1075 nM, Huh7:728.2 nM, NCI-1975:256.3 nM, MDA-MB-231 cells:17.6 nM, Bel-7402:38.4 nM, BGC-803:12.2 nM, Hepa 1-6:32.9 nM, Smmc 7721 cells:12.8 nM
In vitro	Combretastatin A-1 (CA1P) induces apoptosis of TAMs in vitro through the same mechanism observed in HepG2 cells, and it eliminates TAMs in the tumor microenvironment (TME) in vivo. Combretastatin A-1 (1-10 nM; 24 hours) induces AKT inactivation and removal of GSK-3β inhibition by microtubule depolymerization, leading to HepG2 cell apoptosis [2]. Combretastatin A-1 (1-50 nM; 6 hours) reduces the mitochondrial membrane potential (MMP) of HepG2 cells and induces the accumulation of ROS in a dose-dependent manner [3].
In vivo	In the HepG2 subcutaneous xenograft model, Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume [3]. In the orthotopic hepatocellular carcinoma mouse model, Combretastatin A-1 (2 mg/kg; every other day for 21 days) demonstrates enhanced apoptosis [3].

Synonyms	Combretastatin A1
Molecular Weight	332.35
Formula	C18H20O6
CAS No.	109971-63-3

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (240.71 mM), Sonication is recommended.

DMF: 5 mg/mL

Ethanol: 3 mg/mL

DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL

References and Literature

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. 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. 3. 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.

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Keywords

Combretastatin A-1 109971-63-3 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt Microtubule Associated Combretastatin A 1 Combretastatin A1 inhibitor inhibit

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