Tirbanibulin Mesylate (KX01 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).

Src:9 nM (GI50, in HuH7 cells), Src:26 nM(in Hep3B cells), Src:60 nM（in HepG2 cells), Src:13 nM(in PLC/PRF/5 cells)

Tirbanibulin Mesylate is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. Tirbanibulin Mesylate displays steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines [1]. Tirbanibulin Mesylate is evaluated in engineered Src drove cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively [2].

In pre-clinical animal models of cancer, Tirbanibulin Mesylate (p.o.) is shown to inhibit primary tumor growth and to suppress metastasis [2].