| Description | TP-5801 TFA is an orally active inhibitor of TNK1, a non-receptor tyrosine kinase, with an IC50 value of 1.40 nM, demonstrating anti-tumor activity [1]. |
| In vitro | TP-5801 (10 pM-10 μM;72小时) TFA处理有效抑制了TNK1驱动、BCR-ABL驱动和IL-3驱动的Ba/F3细胞增殖[1]。同样,TP-5801 (1 nM-10 μM;10天) TFA可显著抑制TNK1依赖的L540细胞生长[1]。 |
| In vivo | TP-5801 (经口灌胃;10 mg/kg;单次) TFA 在小鼠肿瘤存活模型中表现出疗效[1]。以相同给药方式,TP-5801 (50 mg/kg;每日一次;连续7天) TFA 能有效抑制局部肿瘤生长[1]。 |
| molecular weight | 641.48 |
| Molecular formula | C26H32BrF3N8O3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |