| 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. |
| In vitro | Combretastatin A-1(CA1P)通过相同的机制诱导了体外TAM的凋亡，就像在HepG2细胞中观察到的一样，并且在体内消除了肿瘤微环境(TME)中的TAMs。 Combretastatin A-1(1-10 nM；24小时)通过微管解聚诱导AKT失活和去除GSK-3β抑制，诱导HepG2细胞凋亡[2]。Combretastatin A-1(1-50 nM；6小时)降低了HepG2细胞的线粒体膜电位(MMP)，同时以剂量依赖的方式诱导HepG2细胞中ROS的积累[3]。 |
| In vivo | Combretastatin A-1(1-4 mg/kg；每隔一天静脉注射，持续4周)显著减小了HepG2皮下移植模型中的肿瘤体积[3]。在原位肝细胞癌小鼠模型中，Combretastatin A-1(2 mg/kg；每隔一天，连续21天)显示出增强的凋亡作用[3]。 |
| Target activity | 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 |
| Synonyms | Combretastatin A1 |
| molecular weight | 332.35 |
| Molecular formula | C18H20O6 |
| CAS | 109971-63-3 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | 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 | 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. |