Combretastatin A1 是一种微管聚合抑制剂，可与微管蛋白的秋水仙碱结合位点结合。 Combretastatin A1 通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路。 Combretastatin A1 具有抗肿瘤和抗血管作用。
| Cas No. | 109971-63-3 |
| 别名 | 康普瑞汀A-1 |
| Canonical SMILES | COC(C(O)=C1O)=CC=C1/C=C\C2=CC(OC)=C(OC)C(OC)=C2 |
| 分子式 | C18H20O6 |
| 分子量 | 332.4 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 3 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Combretastatin A1 is a cis-stilbene originally isolated from C. caffrum that inhibits microtubule assembly (ID50 = 2 µM) by binding to the colchicine binding site on β-tubulin. It inhibits proliferation of hepatocellular carcinoma (IC50s = 9.2-728.2 nM) and other carcinoma cell lines (IC50s = 12.2-2,247 nM). Combretastatin A1 increases apoptosis of HepG2 cells in a GSK3β-dependent manner by decreasing the levels of MCL-1 and β-catenin. It inhibits tumor growth in a hepatocellular carcinoma mouse xenograft model when administered at doses of 2 or 4 mg/kg for 4 weeks. It also enhances the effects of carboplatin , paclitaxel , and cisplatin in murine models of cancer. Combretastatin A1 decreases functional vascular volume within hours in a well-vascularized murine colon adenocarcinoma model. |
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