| Description | Colletofragarone A2, isolated from the fungus Colletotrichum sp. (13S020), exhibits anti-cancer activity by inhibiting mutant p53 and HSP90. It promotes the degradation and aggregation of mutant p53, in turn suppressing tumor growth in vivo [1]. |
| In vitro | 突变型p53丧失了原有的肿瘤抑制功能，但在肿瘤进展方面获得了新的能力[1]。Colletofragarone A2（0.05-5 μM；72小时）对p53 R175H结构突变细胞表现出高选择性和更强的细胞毒性活性，相较于其他p53状态如DNA接触突变、野生型和空白细胞[1]。Colletofragarone A2（2 μM；8小时）通过促进p53降解，在SK-BR-3（p53 R175H）细胞中降低突变型p53水平[1]。Colletofragarone A2结合10 μM MG-132（2或4 μM；4小时）诱导突变型p53聚集[1]。 |
| In vivo | Colletofragarone A2（0.35 mM，100 μL，每天肿瘤内注射，持续13天）显著抑制了携带HuCCT1（p53 R175H）细胞的小鼠肿瘤细胞生长[1]。 |
| molecular weight | 386.44 |
| Molecular formula | C22H26O6 |
| CAS | 181377-06-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |