| Description | BT1718 is a bicyclic peptide conjugate that targets MT1-MMP, a protease overexpressed in various advanced solid tumors such as triple-negative breast cancer (TNBC) and non-small cell lung cancer [1] [2]. By exploiting MT1-MMP, BT1718 delivers its cytotoxic payload, Mertansine, with a strong affinity characterized by a dissociation constant (K D) of 3 nM. |
| In vitro | BT1718(IC 50 =1 nM, 72小时)在ATP终点测定中展现了对HT-1080细胞的明显细胞毒性作用[2]。 |
| In vivo | BT1718（10mg/kg，静脉注射，每周三次）在MT1阳性EBC-1细胞植入的小鼠细胞衍生异种移植模型中展现了迅速的肿瘤消减效果[2]。同样的BT1718（10mg/kg，静脉注射，每周一次或两次）在MT1阳性HT-1080细胞植入的小鼠模型中则显示了完全的肿瘤清除效果[2]。 |
| molecular weight | N/A |
| Molecular formula | C159H218ClN31O47S5 |
| CAS | 2227366-66-5 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |