TP-5801 TFA is an orally active inhibitor of TNK1, a non-receptor tyrosine kinase, with an IC50 of 1.40 nM, demonstrating anti-tumor activity [1].

TP-5801 (10 pM-10 μM; 72 h) TFA treatment inhibits the growth of Ba/F3 cells driven by TNK1, BCR-ABL, and IL-3 [1]. Additionally, TP-5801 (1 nM-10 μM; 10 d) TFA suppresses the growth of TNK1-dependent L540 cells [1].

TP-5801, administered via oral gavage at a dose of 10 mg/kg in a single administration, has been shown to be effective in a murine tumor survival model [1]. Moreover, when given at a dose of 50 mg/kg once daily for 7 days, TP-5801 consistently inhibited local tumor growth [1].