Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src , with GI 50 of 9-60 nM in cancer cell lines.
In Vitro
Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 =9 nM), PLC/PRF/5 (GI 50 =13 nM), Hep3B (GI 50 =26 nM), and HepG2 (GI 50 =60 nM), four hepatic cell cancer (HCC) cell lines. Tirbanibulin (KX2-391) 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 (KX2-391) is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI 50 with 23 nM and 39 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
