TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity.IC50 & Target:IC50: 1.40 nM (TNK1)In Vitro:TP-5801 (10?pM-10?μM; 72 h) TFA treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth.
TP-5801 (1?nM-10?μM; 10 d) TFA inhibits TNK1-dependent L540 cell growth.In Vivo:TP-5801 (oral gavage; 10 mg/kg; once) TFA treatment shows efficacy in the mouse survival model.
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) TFA treatment can inhibit localized tumor growth.