| Bioactivity | TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity[1]. |
| Target | IC50: 1.40 nM (TNK1) |
| Invitro | TP-5801 (10 pM-10 μM; 72 h) TFA 处理抑制 TNK1 驱动、BCR-ABL 驱动和 IL-3 驱动的 Ba/F3 细胞生长[1]。TP-5801 (1 nM-10 μM; 10 d) TFA 抑制 TNK1 依赖性 L540 细胞生长[1]。 Cell Viability Assay[1] Cell Line: |
| In Vivo | TP-5801 (oral gavage; 10 mg/kg; once) TFA 在小鼠肿瘤存活模型中有效果[1]。TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) TFA 可抑制局部肿瘤生长[1]。 Animal Model: |
| Name | TP-5801 TFA |
| Formula | C26H32BrF3N8O3 |
| Molar Mass | 641.48 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Tsz-Yin Chan, et al. TNK1 is a ubiquitin-binding and 14-3-3-regulated kinase that can be targeted to block tumor growth. Nat Commun. 2021 Sep 9;12(1):5337. |