Bioactivity | TP-5801 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 mM; 72 h) treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].TP-5801 (1 nM-10 μM; 10 d) inhibits TNK1-dependent L540 cell growth[1]. Cell Viability Assay[1] Cell Line: |
In Vivo | TP-5801 (oral gavage; 10 mg/kg; once) treatment shows efficacy in the mouse survival model[1].TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth[1]. Animal Model: |
Name | TP-5801 |
CAS | 2574474-81-8 |
Formula | C24H31BrN8O |
Molar Mass | 527.46 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
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. |